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 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting | B | 8.97 | pKi | 1.07 | nM | Ki | Bioorg Med Chem (2012) 20: 4556-4563 [PMID:22677527] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig cerebellum | B | 7.35 | pKi | 44.2 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1055-1058 [PMID:20056539] |
| ChEMBL | Binding affinity against Kappa Opioid receptor in Guinea pig brain membranes using [3H]-DAMGO+EKC | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1996) 39: 1816-1822 [PMID:8627605] |
| ChEMBL | Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1991) 34: 1757-1762 [PMID:1648136] |
| ChEMBL | Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 1 | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1990) 33: 1714-1720 [PMID:2160538] |
| ChEMBL | Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of opioid receptor kappa | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1990) 33: 1714-1720 [PMID:2160538] |
| ChEMBL | In vito concentration required to displace 9 (Kd = 1.6 nM and concentration is 1.8 nM) from opioid receptor kappa 1 in guinea brain membranes. | B | 7.77 | pKi | 16.8 | nM | Ki | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Opioid receptor kappa 1 apparent binding constant from guinea pig cerebellum using [3H]diprenorphine binding assay | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1990) 33: 2456-2464 [PMID:2167979] |
| ChEMBL | Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor kappa 1 at temperature 25 degree Celsius labeled with (-)-[3H]immazocine (0.1 nM). | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1985) 28: 974-976 [PMID:2409281] |
| ChEMBL | Binding affinity for Opioid receptor kappa 1 was determined by inhibition of binding of [3H]U-69593 (1.2-2.2 nM) to guinea pig brain membranes | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (1999) 42: 3527-3538 [PMID:10479286] |
| ChEMBL | Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (1993) 36: 2842-2850 [PMID:8410999] |
| ChEMBL | Tested for binding affinity towards kappa receptor in presence of [3H]EKC radioligand | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (1994) 37: 2262-2265 [PMID:8057274] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 of guinea pig brain membranes using 1 nM of (-)-[3H]ethylketazocine as radioligand | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (1986) 29: 1222-1225 [PMID:2879914] |
| ChEMBL | Binding affinity was determined as ability to displace [3H]-U-69, radioligand from Opioid receptor kappa 1 | B | 8.33 | pKi | 4.71 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig membranes | B | 8.33 | pKi | 4.71 | nM | Ki | J Med Chem (1998) 41: 1980-1990 [PMID:9599247] |
| ChEMBL | Binding affinity determined on Opioid receptor kappa 1 in Guinea pig brain membranes using radioligand [3H]U-69593 | B | 8.33 | pKi | 4.71 | nM | Ki | J Med Chem (1998) 41: 5188-5197 [PMID:9857089] |
| ChEMBL | Inhibition of binding of [3H]U69, 593 to Opioid receptor kappa 1 in guinea pig membranes | B | 8.33 | pKi | 4.71 | nM | Ki | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
| ChEMBL | Binding activity against Opioid receptor kappa 1 using [3H]U-69593 as radioligand in guinea pig membranes. | B | 8.33 | pKi | 4.71 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | Binding affinity towards kappa-opioid receptor by displacement of [3H]-EKC at from guinea pig cortical tissue | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1993) 36: 2833-2841 [PMID:8410998] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 using [3H]ethylketocyclazocine as radioligand. | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL |
Binding affinity was determined against Opioid receptor kappa 1 using [3H]ethylketocyclazocine as radioligand |
B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | In vito concentration required to displace 9 (Kd = 1.6 nM and concentration is 1.8 nM) from opioid receptor kappa 1 in guinea brain membranes. | B | 8.55 | pKi | 2.81 | nM | Ki | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by U69,593 to Opioid receptor kappa 1 | F | 8.69 | pKi | 2.06 | nM | Ki | J Med Chem (1998) 41: 1980-1990 [PMID:9599247] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S, binding in guinea pig caudate stimulated by U69,593 in Opioid receptor kappa 1 | F | 8.69 | pKi | 2.05 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | Compound was tested for the inhibition of [35S]GTP-gamma-S, binding to Opioid receptor kappa 1 | F | 8.69 | pKi | 2.05 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor kappa 1 in Guinea pig Caudate stimulated by U69,593 | F | 8.69 | pKi | 2.05 | nM | Ki | J Med Chem (1998) 41: 5188-5197 [PMID:9857089] |
| ChEMBL | Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]U-69593 from Opioid receptor kappa 1 | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1997) 40: 749-753 [PMID:9057861] |
| ChEMBL | Displacement of [3H]U69,593 from guinea pig kappa opioid receptor in cerebellum | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6198-6202 [PMID:21889335] |
| ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in Hartley guinea pig brain membrane | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain homogenate | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Displacement of [3H]-DPN from guinea pig kappa opioid receptor expressed in CHO-K1 cell membranes by radioligand binding assay | B | 9.3 | pKi | 0.5 | nM | Ki | ACS Med Chem Lett (2019) 10: 1641-1647 [PMID:31857840] |
| ChEMBL | Displacement of [3H]U69493 from kappa opioid receptor in Hartley guinea pig cerebellum by liquid scintillation counter | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3726-3729 [PMID:20483601] |
| ChEMBL | Displacement of [3H]U69593 from guinea pig cerebellum kappa opioid receptor | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 121-124 [PMID:19962305] |
| ChEMBL | Displacement of [3H]-U69593 from kappa opioid receptor in guinea pig cerebellum homogenates | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4023-4026 [PMID:21641219] |
| ChEMBL | Binding affinity to kappa opioid receptor in guinea pig cerebellum | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4978-4981 [PMID:18755589] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2416-2419 [PMID:19349178] |
| ChEMBL | Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593 | B | 9.51 | pKi | 0.31 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1717-1721 [PMID:11425545] |
| ChEMBL | Binding affinity was determined towards opioid receptor kappa 1 using [3H]U-69593 as radioligand | B | 9.51 | pKi | 0.31 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1911-1914 [PMID:12749896] |
| ChEMBL | In vito concentration required to displace [3H]BRM (Kd = 1.0 nM and concentration is 1.8 nM) from opioid receptor kappa 2 in guinea brain membranes. | B | 7.33 | pIC50 | 47.2 | nM | IC50 | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane | B | 8.02 | pIC50 | 9.5 | nM | IC50 | J Med Chem (1992) 35: 4589-4594 [PMID:1335078] |
| ChEMBL | Displacement of [3H]bremazocine from opioid receptor kappa of guinea pig membrane. | B | 8.02 | pIC50 | 9.5 | nM | IC50 | J Med Chem (1991) 34: 2438-2444 [PMID:1652019] |
| ChEMBL | Displacement of 0.5 nM [3H]bremazocine from guinea pig brain membrane opioid receptor kappa with 100 nM DAGO and 100 nM DPDPE | B | 8.02 | pIC50 | 9.5 | nM | IC50 | J Med Chem (1992) 35: 2374-2384 [PMID:1320121] |
| ChEMBL | In vito concentration required to displace [3H]BRM (Kd = 1.0 nM and concentration is 1.8 nM) from opioid receptor kappa 2 in guinea brain membranes. | B | 8.22 | pIC50 | 5.97 | nM | IC50 | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Tested for the binding affinity against the Kappa opioid receptor in guinea pig brain using [3H]U-69593 | B | 9.28 | pIC50 | 0.53 | nM | IC50 | J Med Chem (1994) 37: 4270-4277 [PMID:7996538] |
| ChEMBL | Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Activity at human mu opioid receptor by [35S]GTPgammaS binding assay | F | 10.3 | pKd | 0.05 | nM | Kd | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
| ChEMBL | Antagonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of compound 11-induced [35S]GTPgammaS binding | F | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells | B | 8.57 | pKi | 2.71 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by SPA | F | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 670-676 [PMID:21193310] |
| ChEMBL | Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay | B | 8.73 | pKi | 1.85 | nM | Ki | Bioorg Med Chem (2013) 21: 6405-6413 [PMID:24055076] |
| ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 8.78 | pKi | 1.66 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells | B | 8.94 | pKi | 1.15 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2006) 49: 7290-7306 [PMID:17149859] |
| ChEMBL | Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2006) 49: 7278-7289 [PMID:17149858] |
| ChEMBL | Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells in presence of high sodium by SPA | B | 9.06 | pKi | 0.87 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5349-5352 [PMID:17720493] |
| ChEMBL | Displacement of [3H]diprenorphine from cloned human mu opioid receptor expressed in CHO cells | B | 9.06 | pKi | 0.87 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6841-6846 [PMID:17980586] |
| ChEMBL | Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO cells after 1 hr | B | 9.15 | pKi | 0.7 | nM | Ki | Medchemcomm (2013) 4: 847-851 [PMID:23682308] |
| ChEMBL | Radioligand Binding Assay: A bivalent ligand 1 (FIG. 14) that combines the pharmacophores of naltrexone (a MOR antagonist) and maraviroc (a CCR5 antagonist) into one molecule was designed and synthesized. Herein is reported the characterization of this novel molecular probe in for its binding affinity, Ca2− flux functional activity, and HIV-1 inhibition potency. Bivalent ligand 1 was first characterized in hMOR-expressed CHO cells in the competitive radioligand binding assay as described previously. | B | 9.15 | pKi | 0.7 | nM | Ki | US-9107954-B2. Bivalent ligands for the treatment of neurological disorders (2015) |
| ChEMBL | Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 9.23 | pKi | 0.59 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5349-5352 [PMID:17720493] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 using [3H]naloxone as radioligand. | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in HEK cells after 60 mins | B | 9.35 | pKi | 0.45 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
| ChEMBL | Displacement of [3H]naloxone from mu opioid receptor (unknown origin) after 1.5 hrs | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3719-3722 [PMID:23721804] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexyl)-amino)-6-oxohexyl)-3,3-dimethyl-3H-indol-1-ium-5-sulfonate,2,2,2-Trifluoroacetate Salt from human MOR expressed in HEK293 cells by Cheng-Prusoff analysis | B | 9.56 | pKi | 0.28 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells | B | 9.59 | pKi | 0.26 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280] |
| ChEMBL | Displacement of [3H]NLX from mu opioid receptor (unknown origin) expressed in CHO cell membranes after 1.5 hrs | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (2013) 56: 9156-9169 [PMID:24144240] |
| ChEMBL | Displacement of [3H]naloxone from monocloned mu opioid receptor expressed in CHO cells | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (2009) 52: 1416-1427 [PMID:19199782] |
| ChEMBL | Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells | B | 9.64 | pKi | 0.23 | nM | Ki | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 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 for human Opioid receptor mu 1 transfected into chinese hamster ovary cells by displacing [3H]DAMGO radioligand | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2003) 46: 3174-3177 [PMID:12825957] |
| ChEMBL | Inhibition of [3H]DAMGO binding to human Mu opioid receptor expressed in CHO cells | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2004) 47: 5069-5075 [PMID:15456250] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cells | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Displacement of [3H]DAMGO from human cloned mu opioid receptor | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu 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] |
| GtoPdb | - | - | 9.7 | pKi | 0.2 | nM | Ki |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Psychopharmacology (Berl.) (2015) 232: 305-14 [PMID:24973897] |
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| ChEMBL | Displacement of [3H]-DPN from recombinant human mu opioid receptor expressed in CHO-K1 cell membranes by radioligand binding assay | B | 9.8 | pKi | 0.16 | nM | Ki | ACS Med Chem Lett (2019) 10: 1641-1647 [PMID:31857840] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting | B | 9.96 | pKi | 0.11 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells | B | 9.96 | pKi | 0.11 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 expressed in CHO cells using [3H]DAMGO as radioligand | B | 9.96 | pKi | 0.11 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2107-2110 [PMID:15808478] |
| ChEMBL | Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells | B | 10.15 | pKi | 0.07 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as inhibition of DAGO-stimulated [35S]GTPgammaS binding | F | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Antagonist activity at human MOR expressed in CHO cells assessed as inhibition of DAMGO-induced increase in intracellular Ca2+ level incubated for 15 mins prior to DAMGO addition by microplate reader analysis | F | 7.81 | pIC50 | 15.5 | nM | IC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| ChEMBL | Flux Assay: As Ca2+ flux is associated with the activation of the MOR, the functional activity of bivalent ligand 1, monovalent ligand 2, and naltrexone was then evaluated in a Ca2+ mobilization assay in hMORCHO cells transfected with chimeric Ca2+ following a published protocol.23 No agonism was observed for any of the tested compounds (data not shown). Thus, they were further assessed for their antagonist properties as the ability to inhibit DAMGO (a MOR agonist) induced Ca2+ flux. | F | 8.05 | pIC50 | 8.9 | nM | IC50 | US-9107954-B2. Bivalent ligands for the treatment of neurological disorders (2015) |
| ChEMBL | Antagonist activity at human mu opioid receptor expressed in CHO cells co- expressing Gqi5 assessed as decrease in DAMGO-induced intracellular calcium mobilization incubated for 15 mins followed by DAMGO addition by Fluo-AM dye based fluorescence assay | F | 8.05 | pIC50 | 8.9 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2318-2324 [PMID:33214847] |
| ChEMBL | Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge | F | 8.05 | pIC50 | 8.9 | nM | IC50 | Medchemcomm (2013) 4: 847-851 [PMID:23682308] |
| ChEMBL | Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding | F | 8.32 | pIC50 | 4.8 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells | F | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2006) 49: 7290-7306 [PMID:17149859] |
| ChEMBL | Antagonist activity against human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding | F | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2006) 49: 7278-7289 [PMID:17149858] |
| ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 8.39 | pIC50 | 4.08 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay | B | 8.41 | pIC50 | 3.9 | nM | IC50 | Bioorg Med Chem (2013) 21: 6405-6413 [PMID:24055076] |
| ChEMBL | Antagonist activity at human MOR transfected in CHO cells co-transfected with Gqi5 assessed as inhibition of DAMGO-induced calcium mobilization incubated for 15 mins prior to DAMGO addition and measured for 90 secs by Fluo-4AM dye based fluorescence analysis | F | 8.54 | pIC50 | 2.87 | nM | IC50 | Bioorg Med Chem (2016) 24: 5969-5987 [PMID:27720326] |
| ChEMBL | Activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 9.23 | pIC50 | 0.59 | nM | IC50 | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.8 | pEC50 | 16 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Effective concentration agonistic activity towards Opioid receptor mu 1 | F | 9.23 | pEC50 | 0.59 | nM | EC50 | J Med Chem (2003) 46: 3174-3177 [PMID:12825957] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding | B | 9.42 | pEC50 | 0.38 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 3719-3722 [PMID:23721804] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Antagonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as reversal of Sufentanil effect on electrically-induced driven twitch | F | 8.76 | pKd | 1.74 | nM | Kd | Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026] |
| ChEMBL | Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay | B | 8.31 | pKi | 4.91 | nM | Ki | Bioorg Med Chem (2013) 21: 6405-6413 [PMID:24055076] |
| ChEMBL | Displacement of [3H]-naloxone from mouse MOR expressed in CHO cells incubated for 1.5 hrs by competitive radioligand binding assay | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2021) 64: 7702-7723 [PMID:34027668] |
| ChEMBL | Displacement of [3H]-DAMGO from mouse MOR expressed in HEK293 cells | B | 9.19 | pKi | 0.65 | nM | Ki | ACS Med Chem Lett (2012) 3: 640-644 [PMID:23585918] |
| ChEMBL | Displacement of [3H]-NLX from mouse mu opioid receptor expressed in CHO cells measured after 1.5 hrs by competitive-binding assay | B | 9.4 | pKi | 0.4 | nM | Ki | ACS Med Chem Lett (2020) 11: 2318-2324 [PMID:33214847] |
| ChEMBL | Displacement of [3H]NLX from mouse MOR expressed in CHO cell membrane incubated for 90 mins by liquid scintillation spectrophotometry | B | 9.41 | pKi | 0.39 | nM | Ki | Bioorg Med Chem (2016) 24: 5969-5987 [PMID:27720326] |
| ChEMBL | Displacement of [3H]-NLX from mouse MOR expressed in CHO cells incubated for 1.5 hrs by radioligand binding assay | B | 9.41 | pKi | 0.39 | nM | Ki | RSC Med Chem (2020) 11: 125-131 [PMID:33479612] |
| ChEMBL | Displacement of [3H]naloxane from mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 9.48 | pKi | 0.33 | nM | Ki | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| ChEMBL | Displacement of [3H]-naloxone from mouse mu opioid receptor expressed in CHO cells after 1.5 hrs | B | 9.48 | pKi | 0.33 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5045-5048 [PMID:23948248] |
| ChEMBL | Displacement of [3H]DAMGO from mouse mu opioid receptor in whole brain without cerebellum | B | 9.58 | pKi | 0.27 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6198-6202 [PMID:21889335] |
| ChEMBL | Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay | B | 7.99 | pIC50 | 10.35 | nM | IC50 | Bioorg Med Chem (2013) 21: 6405-6413 [PMID:24055076] |
| ChEMBL | Antagonist activity at mouse MOR expressed in CHO cells assessed as inhibition of DAMGO-induced calcium mobilization preincubated for 60 mins measured after 15 mins by calcium mobilization assay | F | 8.18 | pIC50 | 6.62 | nM | IC50 | J Med Chem (2021) 64: 7702-7723 [PMID:34027668] |
| ChEMBL | Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs | F | 9.8 | pEC50 | 0.16 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5045-5048 [PMID:23948248] |
| ChEMBL | Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 9.8 | pEC50 | 0.16 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | In vito concentration required to displace [3H]cyclofoxy (Kd = 0.8 nM and concentration is 1.3 nM) from mu and kappa2 receptor in rat brain membranes. | B | 8.59 | pKi | 2.57 | nM | Ki | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Binding affinity for Opioid receptor mu 1 was determined by inhibition of binding of [3H]DAMGO (1.4-3 nM) to rat brain membranes | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (1999) 42: 3527-3538 [PMID:10479286] |
| ChEMBL | Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1 | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1990) 33: 2456-2464 [PMID:2167979] |
| ChEMBL | Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2001) 44: 857-862 [PMID:11300867] |
| ChEMBL | Binding affinity was determined as ability to displace [3H]DAMGO radioligand from Mu opioid receptor | B | 8.86 | pKi | 1.39 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 8.86 | pKi | 1.39 | nM | Ki | J Med Chem (1998) 41: 1980-1990 [PMID:9599247] |
| ChEMBL | Binding activity against Opioid receptor mu 1 using [3H]DAMGO as radioligand in rat brain membranes. | B | 8.86 | pKi | 1.39 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | In vito concentration required to displace [3H]DAGO (Kd = 0.7 nM and concentration is 1.7 nM) from opioid receptor mu in rat brain membranes. | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (1993) 36: 2842-2850 [PMID:8410999] |
| ChEMBL | Tested for binding affinity towards mu receptor in presence of [3H]NAL radioligand | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (1994) 37: 2262-2265 [PMID:8057274] |
| ChEMBL | Binding affinity towards mu opioid receptor by displacement of [3H]NAL from rat brain homogenates | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (1993) 36: 2833-2841 [PMID:8410998] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting | B | 9.34 | pKi | 0.46 | nM | Ki | Bioorg Med Chem (2012) 20: 4556-4563 [PMID:22677527] |
| ChEMBL | In vito concentration required to displace [3H]cyclofoxy (Kd = 0.8 nM and concentration is 1.3 nM) from mu and kappa2 receptor in rat brain membranes. | B | 8.17 | pIC50 | 6.77 | nM | IC50 | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | In vito concentration required to displace [3H]DAGO (Kd = 0.7 nM and concentration is 1.7 nM) from opioid receptor mu in rat brain membranes. | B | 8.39 | pIC50 | 4.04 | nM | IC50 | J Med Chem (1992) 35: 2826-2835 [PMID:1322988] |
| ChEMBL | Evaluated for the inhibition of [3H]naltrexone binding to Opioid receptor mu 1 in rat brain homogenates. | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (1985) 28: 1950-1953 [PMID:2999408] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Inhibition of binding of [3H]DAMGO to Opioid receptor mu 1 in guinea pig membranes | B | 8.86 | pKi | 1.39 | nM | Ki | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
| ChEMBL | Binding affinity determined on Opioid receptor mu 1 in Guinea pig brain membranes using radioligand [3H]DAMGO | B | 8.86 | pKi | 1.39 | nM | Ki | J Med Chem (1998) 41: 5188-5197 [PMID:9857089] |
| ChEMBL | Inhibitory binding constant in guinea pig brain homogenate was reported at mu site at a temperature 25 degree Centigrade labeled with [3H](D-Ala2-MePhe4,Gly-ol5)enkephalin(1 nM) | B | 8.97 | pKi | 1.08 | nM | Ki | J Med Chem (1985) 28: 974-976 [PMID:2409281] |
| ChEMBL | Compound was tested for the inhibition of [35S]GTP-gamma-S, binding in Guinea pig Caudate stimulated by the opioid receptor agonist Mu-DAMGO | F | 9.03 | pKi | 0.93 | 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 to Opioid receptor mu 1 in Guinea pig caudate stimulated by DAMGO[mu] | F | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (1998) 41: 1980-1990 [PMID:9599247] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor mu 1 in Guinea pig Caudate stimulated by DAMGO | F | 9.03 | pKi | 0.93 | 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 DAMGO (Opioid receptor mu 1) | F | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (1998) 41: 4143-4149 [PMID:9767649] |
| ChEMBL | Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 1 | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1990) 33: 1714-1720 [PMID:2160538] |
| ChEMBL | Compound was evaluated for binding affinity at Opioid receptor mu 1 in guinea pig brain membranes | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1991) 34: 1757-1762 [PMID:1648136] |
| ChEMBL | Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of opioid receptor mu | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1990) 33: 1714-1720 [PMID:2160538] |
| ChEMBL | Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]DAMGO from Opioid receptor mu 1 | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1997) 40: 749-753 [PMID:9057861] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 in Guinea pig brain membranes using [3H]DAMGO | B | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (1996) 39: 1816-1822 [PMID:8627605] |
| ChEMBL | Binding affinity was determined against Mu opioid receptor using [3H]naltrexone as radioligand | B | 9.25 | pKi | 0.56 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3149-3152 [PMID:9873693] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain homogenate | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2006) 49: 6104-6110 [PMID:17004724] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Hartley guinea pig brain membrane | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 of guinea pig brain membranes using 0.5 nM of [3H]naloxone as radioligand | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (1986) 29: 1222-1225 [PMID:2879914] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Hartley guinea pig forebrain by liquid scintillation counting | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3726-3729 [PMID:20483601] |
| ChEMBL | Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig forebrain homogenates | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4023-4026 [PMID:21641219] |
| ChEMBL | Binding affinity to mu opioid receptor in guinea pig forebrain | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4978-4981 [PMID:18755589] |
| ChEMBL | Displacement of [3H]DAMGO from guinea pig forebrain mu opioid receptor | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 121-124 [PMID:19962305] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1055-1058 [PMID:20056539] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain | B | 9.49 | pKi | 0.33 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2416-2419 [PMID:19349178] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membrane | B | 9.59 | pKi | 0.26 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 2074-2078 [PMID:28291693] |
| ChEMBL | Binding affinity was determined towards opioid receptor mu1 using [3H]DAMGO as radioligand | B | 9.77 | pKi | 0.17 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1911-1914 [PMID:12749896] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 of guinea pig brain membranes using radioligand 0.25 nM [3H]DAMGO | B | 9.77 | pKi | 0.17 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1717-1721 [PMID:11425545] |
| ChEMBL | Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane | B | 9.14 | pIC50 | 0.73 | nM | IC50 | J Med Chem (1992) 35: 4589-4594 [PMID:1335078] |
| ChEMBL | inhibition of 1.0 nM [3H]- DAGO binding to guinea pig brain membrane opioid receptor mu | B | 9.14 | pIC50 | 0.73 | nM | IC50 | J Med Chem (1992) 35: 2374-2384 [PMID:1320121] |
| ChEMBL | Tested for the binding affinity against the Mu opioid receptor in guinea pig brain using [3H]-DAMGO | B | 9.64 | pIC50 | 0.23 | nM | IC50 | J Med Chem (1994) 37: 4270-4277 [PMID:7996538] |
| ChEMBL | Inhibitory concentration was determined against Opioid receptor mu 1 using [3H]- DAMGO radioligand | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL307] [GtoPdb: 465] [UniProtKB: P09483] | ||||||||
| ChEMBL | Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in acute hippocampal slices | B | 4.51 | pIC50 | 31000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1879-1887 [PMID:15050620] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in cultured hippocampal neurons | B | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1879-1887 [PMID:15050620] |
| ChEMBL | Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in hippocampal primary cultures | B | 4.6 | pIC50 | 25000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1879-1887 [PMID:15050620] |
| NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
| ChEMBL | Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding | F | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
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]
