naltrexone [Ligand Id: 1639] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19019 (Celupan, EN-1639A, EN-1639A [AS HYDROCHLORIDE], EN-1639A FREE BASE, Naltrexone, NSC-758439, Revia, Trexal, Trexan, Vivitrol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6 | pIC50 | 1000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Activity at human delta opioid receptor by [35S]GTPgammaS binding assay | F | 8.8 | pKd | 1.58 | nM | Kd | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
| ChEMBL | Displacement of [3H]NTI from monocloned delta opioid receptor expressed in CHO cells | B | 6.93 | pKi | 117.06 | nM | Ki | J Med Chem (2009) 52: 1416-1427 [PMID:19199782] |
| ChEMBL | Displacement of [3H]NTI from delta opioid receptor expressed in CHO cells | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280] |
| ChEMBL | Displacement of [3H]NTI from delta opioid receptor (unknown origin) expressed in CHO cell membranes after 1.5 hrs | B | 7.02 | pKi | 95.5 | nM | Ki | J Med Chem (2013) 56: 9156-9169 [PMID:24144240] |
| ChEMBL | Displacement of [3H]NTI from delta opioid receptor (unknown origin) after 1.5 hrs | B | 7.02 | pKi | 95.46 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3719-3722 [PMID:23721804] |
| ChEMBL | Binding affinity determined on Opioid receptor delta 1 in Guinea pig brain membranes using radioligand [3H]DADLE | B | 7.02 | pKi | 94.9 | nM | Ki | J Med Chem (1998) 41: 5188-5197 [PMID:9857089] |
| ChEMBL | Inhibition of binding of [3H]DADLE to Opioid receptor delta 1 in guinea pig membranes | B | 7.02 | pKi | 94.9 | nM | Ki | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
| ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 7.06 | pKi | 88 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of compound 14-induced [35S]GTPgammaS binding | F | 7.18 | pKi | 66.8 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 expressed in CHO cells using [3H]Naltrindole as radioligand | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2107-2110 [PMID:15808478] |
| ChEMBL | Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Displacement of [3H]naltrindole from human opioid delta receptor expressed in CHO cells | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1991) 34: 1757-1762 [PMID:1648136] |
| ChEMBL | Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 1 | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1990) 33: 1714-1720 [PMID:2160538] |
| ChEMBL | Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of opioid receptor delta | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1990) 33: 1714-1720 [PMID:2160538] |
| ChEMBL | Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by SPA | F | 7.6 | pKi | 25.12 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 670-676 [PMID:21193310] |
| ChEMBL | Binding affinity against Delta Opioid receptor in Guinea pig brain membranes using [3H]DAMGO+DADLE | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1996) 39: 1816-1822 [PMID:8627605] |
| ChEMBL | Compound was tested for the inhibition of [35S]GTP-gamma-S, binding in Guinea pig Caudate stimulated by the Opioid receptor delta 1 agonist Delta-SNC80 | F | 7.71 | pKi | 19.3 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by SMC-80 (Opioid receptor delta 1) | F | 7.71 | pKi | 19.3 | nM | Ki | J Med Chem (1998) 41: 1980-1990 [PMID:9599247] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor delta 1 in Guinea pig Caudate stimulated by SNC80 | F | 7.71 | pKi | 19.3 | nM | Ki | J Med Chem (1998) 41: 5188-5197 [PMID:9857089] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S, binding in guinea pig caudate stimulated by SNC80 (Opioid receptor delta 1) | F | 7.71 | pKi | 19.3 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | Displacement of [3H]bremazocine from human delta opioid receptor expressed in CHO cells in presence of high sodium by SPA | B | 7.79 | pKi | 16.31 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5349-5352 [PMID:17720493] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells | B | 7.79 | pKi | 16.31 | nM | Ki | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
| ChEMBL | Displacement of [3H]bremazocine from cloned human delta opioid receptor expressed in CHO cells | B | 7.79 | pKi | 16.31 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6841-6846 [PMID:17980586] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 7.79 | pKi | 16.31 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2006) 49: 7278-7289 [PMID:17149858] |
| ChEMBL | Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2006) 49: 7290-7306 [PMID:17149859] |
| ChEMBL | Antagonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 7.96 | pKi | 11.06 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5349-5352 [PMID:17720493] |
| ChEMBL | Binding affinity was determined towards Opioid receptor delta 1 using [3H]naltrindole as radioligand | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1911-1914 [PMID:12749896] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]DPDPE from Opioid receptor delta 1 | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (1997) 40: 749-753 [PMID:9057861] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 of guinea pig brain membranes using radioligand 0.2 nM [3H]Naltrindole | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1717-1721 [PMID:11425545] |
| ChEMBL | Inhibition of [3H]C1-DPDPE binding to human delta opioid receptor expressed in CHO cells | B | 7.97 | pKi | 10.8 | 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 cells | B | 7.97 | pKi | 10.8 | nM | Ki | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Displacement of [3H]DPDPE from human cloned delta opioid receptor | B | 7.97 | pKi | 10.8 | nM | Ki | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
| ChEMBL | Displacement of [3H]Cl-DPDPE from human recombinant DOR expressed in CHO cells | B | 7.97 | pKi | 10.8 | nM | Ki | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
| 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 | 7.97 | pKi | 10.8 | nM | Ki | Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818] |
| ChEMBL | Binding affinity for human Opioid receptor delta 1 transfected into chinese hamster ovary cells by displacing [3H]CI-DPDPE radioligand | B | 7.97 | pKi | 10.8 | nM | Ki | J Med Chem (2003) 46: 3174-3177 [PMID:12825957] |
| ChEMBL | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | B | 7.97 | pKi | 10.8 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| GtoPdb | - | - | 8 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 of guinea pig brain membranes using 1 nM of [3H]DADLE as radioligand | B | 8.03 | pKi | 9.4 | nM | Ki | J Med Chem (1986) 29: 1222-1225 [PMID:2879914] |
| ChEMBL | Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor delta 1 at a a temperature 25 degree Celsius labeled with [3H](D-Ala2-D-Leu5)-enkephalin (0.7 nM) | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (1985) 28: 974-976 [PMID:2409281] |
| ChEMBL | Displacement of [3H]Cl-DPDPE from delta receptor in guinea pig brain homogenate | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Displacement of [3H]-DPN from recombinant human delta opioid receptor expressed in CHO-K1 cell membranes by radioligand binding assay | B | 8.2 | pKi | 6.31 | nM | Ki | ACS Med Chem Lett (2019) 10: 1641-1647 [PMID:31857840] |
| ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 6.6 | pIC50 | 251 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding | F | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Inhibition of [3H]DPDPE binding to guinea pig brain membrane Opioid receptor delta 1 at 1.0 nM | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1992) 35: 2374-2384 [PMID:1320121] |
| ChEMBL | Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1992) 35: 4589-4594 [PMID:1335078] |
| ChEMBL | Tested for the binding affinity against the Delta opioid receptor in guinea pig brain using [3H]DPDPE | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1994) 37: 4270-4277 [PMID:7996538] |
| ChEMBL | Inhibitory concentration was determined against delta-opioid receptor using [3H]- DPDPE radioligand | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| ChEMBL | Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 8.26 | pIC50 | 5.44 | nM | IC50 | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.68 | pEC50 | 21 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Agonistic activity towards Opioid receptor delta 1 | F | 8.26 | pEC50 | 5.44 | nM | EC50 | J Med Chem (2003) 46: 3174-3177 [PMID:12825957] |
| ChEMBL | Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay | F | 8.26 | pEC50 | 5.44 | nM | EC50 | Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818] |
| ChEMBL | Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs | F | 8.36 | pEC50 | 4.4 | nM | EC50 | J Med Chem (2013) 56: 9156-9169 [PMID:24144240] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Antagonist activity at delta opioid receptor in Swiss mouse vas deferens assessed as reversal of DSLET effect on electrically-induced driven twitch | F | 7.41 | pKd | 38.9 | nM | Kd | Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| ChEMBL | Displacement of [3H]-naltrindole from mouse delta opioid receptor expressed in CHO cells after 1.5 hrs | B | 6.84 | pKi | 143.5 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5045-5048 [PMID:23948248] |
| ChEMBL | Displacement of [3H]naltrindole from mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 6.84 | pKi | 143.5 | nM | Ki | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| ChEMBL | Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells | B | 7.25 | pKi | 55.7 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Displacement of [3H]- diprenorphine from delta-receptor expressed in HEK 293 cells | B | 7.35 | pKi | 44.7 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Displacement of [3H]DPDPE from mouse delta opioid receptor in whole brain without cerebellum | B | 7.91 | pKi | 12.27 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6198-6202 [PMID:21889335] |
| ChEMBL | Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 8.36 | pEC50 | 4.4 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | In vito concentration required to displace [3H]DADLE (Kd = 1.6 nM and concentration is 1.9 nM) from high affinity delta-site in rat brain membranes. | B | 7 | pKi | 101 | nM | Ki | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain membranes | B | 7.02 | pKi | 94.9 | nM | Ki | J Med Chem (1998) 41: 1980-1990 [PMID:9599247] |
| ChEMBL | Binding affinity was determined as ability to displace [3H]DADLE radioligand from Opioid receptor delta 1 | B | 7.02 | pKi | 94.9 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | Binding activity against Opioid receptor delta 1 using [3H]DADLE as radioligand in rat brain membranes. | B | 7.02 | pKi | 94.9 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | Binding affinity for Opioid receptor delta 1 was determined by inhibition of binding of [3H]DADLE (1.3-2.0 nM) to rat brain membranes | B | 7.4 | pKi | 39.5 | nM | Ki | J Med Chem (1999) 42: 3527-3538 [PMID:10479286] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem (2012) 20: 4556-4563 [PMID:22677527] |
| ChEMBL | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Opioid receptor delta 1 apparent binding constant from rat brain membranes using [3H]DADLE binding assay | B | 8.17 | pKi | 6.7 | nM | Ki | J Med Chem (1990) 33: 2456-2464 [PMID:2167979] |
| ChEMBL | In vito concentration required to displace [3H]DADLE (Kd = 12.2 nM and concentration is 2.1 nM) from low affinity delta-site in rat brain membranes. | B | 8.32 | pKi | 4.75 | nM | Ki | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | In vito concentration required to displace [3H]DADLE (Kd = 1.6 nM and concentration is 1.9 nM) from high affinity delta-site in rat brain membranes. | B | 6.66 | pIC50 | 221 | nM | IC50 | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | In vito concentration required to displace [3H]-DADLE (Kd = 12.2 nM and concentration is 2.1 nM) from low affinity delta-site in rat brain membranes. | B | 8.25 | pIC50 | 5.57 | nM | IC50 | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by SPA | F | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 670-676 [PMID:21193310] |
| ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 8.14 | pKi | 7.17 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]diprenorphine from cloned human kappa opioid receptor expressed in CHO cells | B | 8.28 | pKi | 5.28 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6841-6846 [PMID:17980586] |
| ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells in presence of high sodium by SPA | B | 8.28 | pKi | 5.28 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5349-5352 [PMID:17720493] |
| ChEMBL | Displacement of [3H]norBNI from monocloned kappa opioid receptor expressed in CHO cells | B | 8.29 | pKi | 5.15 | nM | Ki | J Med Chem (2009) 52: 1416-1427 [PMID:19199782] |
| ChEMBL | Displacement of [3H]norBNI from kappa opioid receptor expressed in CHO cells | B | 8.29 | pKi | 5.15 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280] |
| ChEMBL | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (2006) 49: 7290-7306 [PMID:17149859] |
| ChEMBL | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (2006) 49: 7278-7289 [PMID:17149858] |
| ChEMBL | Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 8.52 | pKi | 2.99 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5349-5352 [PMID:17720493] |
| ChEMBL | Displacement of [3H]DPN from kappa opioid receptor (unknown origin) after 1.5 hrs | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3719-3722 [PMID:23721804] |
| ChEMBL | Displacement of [3H]DPN from kappa opioid receptor (unknown origin) expressed in CHO cell membranes after 1.5 hrs | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2013) 56: 9156-9169 [PMID:24144240] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 9.09 | pKi | 0.81 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
| ChEMBL | Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818] |
| ChEMBL | Binding affinity in recombinant human Opioid receptor kappa 1 transfected into chinese hamster ovary cells by displacing [3H]U-69593 radioligand | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2003) 46: 3174-3177 [PMID:12825957] |
| ChEMBL | Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2004) 47: 5069-5075 [PMID:15456250] |
| ChEMBL | Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
| ChEMBL | Displacement of [3H]U-69593 from human recombinant kappa opioid receptor expressed in CHO cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Displacement of [3H]U-69593 from human cloned kappa opioid receptor | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
| ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| GtoPdb | - | - | 9.4 | 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); Proc Natl Acad Sci USA (1995) 92: 7006-10 [PMID:7624359] |
| ChEMBL | Displacement of [3H]U-69593 from human opioid kappa receptor expressed in CHO cells | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 expressed in CHO cells using [3H]U-69593 as radioligand | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2107-2110 [PMID:15808478] |
| ChEMBL | Antagonist activity at kappa opioid receptor expressed in HEK293 cells assessed as inhibition of compound 16-induced [35S]GTPgammaS binding | F | 10.38 | pKi | 0.04 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding | F | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding | F | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 7.74 | pIC50 | 18 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 8.73 | pIC50 | 1.86 | nM | IC50 | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.48 | pEC50 | 3.3 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Agonistic activity towards Opioid receptor kappa 1 | F | 8.73 | pEC50 | 1.86 | nM | EC50 | J Med Chem (2003) 46: 3174-3177 [PMID:12825957] |
| ChEMBL | Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs | F | 9.09 | pEC50 | 0.81 | nM | EC50 | J Med Chem (2013) 56: 9156-9169 [PMID:24144240] |
| ChEMBL | Activity at human kappa opioid receptor by [35S]GTPgammaS binding assay | F | 9.68 | pA2 | 9.68 | nM | pA2 | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Antagonist activity at kappa opioid receptor in Swiss mouse vas deferens assessed as reversal of U50488 effect on electrically-induced driven twitch | F | 7.74 | pKd | 18.2 | nM | Kd | Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026] |
| ChEMBL | Displacement of [3H]-diprenorphine from mouse kappa opioid receptor expressed in CHO cells after 1.5 hrs | B | 8.84 | pKi | 1.44 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5045-5048 [PMID:23948248] |
| ChEMBL | Displacement of [3H]diprenorphine from mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 8.84 | pKi | 1.44 | nM | Ki | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| GtoPdb | - | - | 9.2 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575] |
| ChEMBL | Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 9.09 | pEC50 | 0.81 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells | B | 7.9 | pKi | 12.7 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells | B | 8.74 | pKi | 1.8 | |||