[3H]naltrindole [Ligand Id: 3829] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL567175 (Naltrindole)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
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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 Antagonist activity against delta opioid receptor assessed as effect on deltorphin-2-induced calcium response in CHO cells by aequorin luminescence based calcium assay F 7.95 pKd 11.22 nM Kd J. Med. Chem. (2007) 50: 512-520 [PMID:17266203]
ChEMBL Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells B 8.71 pKi 1.97 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL Displacement of [3H]DADLE from delta opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay B 9.05 pKi 0.9 nM Ki Eur. J. Med. Chem. (2014) 85: 818-829 [PMID:25193297]
ChEMBL Displacement of [3H]DADLE from delta opioid receptor (unknown origin) B 9.05 pKi 0.9 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2860-2862 [PMID:23587424]
ChEMBL Displacement of [125I]-IBNalA from DOR-1 expressed in CHO cells B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [125I]-IBNtxA from DOR-1 expressed in CHO cells B 9.34 pKi 0.46 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [3H]DPDPE from human DOR expressed in CHO cells B 9.34 pKi 0.46 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL Binding affinity determined against Opioid receptor delta 1 from human cloned receptor B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of [3H]DADLE from Opioid receptor delta 1 B 9.66 pKi 0.22 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2883-2885 [PMID:11597422]
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 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Inhibition of [3H]C1-DPDPE binding to human delta opioid receptor expressed in CHO cells B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL Binding affinity for human Opioid receptor delta 1 transfected into chinese hamster ovary cells by displacing [3H]CI-DPDPE radioligand B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2003) 46: 3174-3177 [PMID:12825957]
ChEMBL Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cells B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2004) 47: 6645-6648 [PMID:15588100]
ChEMBL Binding affinity towards recombinant human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta) B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2002) 45: 537-540 [PMID:11784158]
ChEMBL Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig B 9.8 pKi 0.16 nM Ki J. Med. Chem. (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of [3H]Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells after 60 mins B 9.8 pKi 0.16 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Binding affinity to Opioid receptor delta 1 using [3H]DPDPE as a radioligand in guinea pig B 9.82 pKi 0.15 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 939-943 [PMID:11294396]
ChEMBL Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting B 9.85 pKi 0.14 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL Displacement of [3H]diprenorphine from human recombinant delta opioid receptor expressed in in CHO cells B 9.97 pKi 0.11 nM Ki Bioorg. Med. Chem. (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL [3H]-Cl-DPDPE competition binding assay using human cloned opioid receptor delta 1 B 10.15 pKi 0.07 nM Ki J. Med. Chem. (2004) 47: 281-284 [PMID:14711299]
ChEMBL Ability to inhibit GTP-gamma-S binding to Opioid receptor delta 1 of guinea pig caudate. B 10.21 pKi 0.06 nM Ki J. Med. Chem. (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL Apparent antagonist activity determined by measuring the ability to inhibit stimulation of [35S]GTP-gamma-S, binding to opioid receptor delta 1 in guinea pig caudate membranes F 10.21 pKi 0.06 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by SNC80 (Opioid receptor delta 1) antagonist F 10.21 pKi 0.06 nM Ki J. Med. Chem. (2002) 45: 5378-5383 [PMID:12431065]
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 10.4 pKi 0.04 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 529-532 [PMID:12565965]
ChEMBL Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes B 10.51 pKi 0.03 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 B 10.52 pKi 0.03 nM Ki J. Med. Chem. (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL The compound was evaluated for binding affinity against Opioid receptor delta 1 in guinea pig brain membrane using [3H]- DPDPE as ligand B 10.52 pKi 0.03 nM Ki J. Med. Chem. (1992) 35: 4325-4329 [PMID:1333013]
ChEMBL The opioid receptor affinity(Ki) was evaluated by competition with [3H]-DPDPE (delta 1) on guinea pig brain membranes B 10.52 pKi 0.03 nM Ki J. Med. Chem. (1995) 38: 402-407 [PMID:7853332]
ChEMBL Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 1 B 10.52 pKi 0.03 nM Ki J. Med. Chem. (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL Displacement of [3H]Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells after 60 mins B 9.04 pIC50 0.91 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as reduction in SNC80-induced inhibition of forskolin stimulated cAMP accumulation preincubated for 15 mins followed SNC80 and forskolin addition and measured after 10 mins relative to control B 9.29 pIC50 <0.51 nM IC50 ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding F 9.41 pIC50 0.39 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane B 9.49 pIC50 0.32 nM IC50 J. Med. Chem. (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL Agonistic activity towards Opioid receptor delta 1 F 9.96 pEC50 0.11 nM EC50 J. Med. Chem. (2003) 46: 3174-3177 [PMID:12825957]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of deltorphin-II from delta opioid receptor in mouse vas deferens B 9.2 pKd 0.63 nM Kd J. Med. Chem. (2005) 48: 8035-8044 [PMID:16335927]
ChEMBL Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells B 8.74 pKi 1.82 nM Ki J. Med. Chem. (2001) 44: 857-862 [PMID:11300867]
ChEMBL Binding affinity against Opioid receptor delta 1 using [3H][D-Ala2, D-Leu5]-enkephalin as radioligand B 9.3 pKi 0.5 nM Ki J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL Displacement of [3H]- diprenorphine from delta receptor expressed in HEK 293 cells B 9.72 pKi 0.19 nM Ki J. Med. Chem. (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum B 9.77 pKi 0.17 nM Ki Bioorg. Med. Chem. (2012) 20: 5810-5831 [PMID:22967810]
ChEMBL Displacement of [3H]NTI from delta opioid receptor in CD1 mouse brain membranes B 9.82 pKi 0.15 nM Ki J. Med. Chem. (2007) 50: 2144-2156 [PMID:17402725]
ChEMBL Binding affinity against Opioid receptor delta 1 receptor binding in ICR mouse brain membranes using the radioligand [3H]naltrindole B 10.4 pKi 0.04 nM Ki J. Med. Chem. (1997) 40: 1977-1981 [PMID:9207938]
ChEMBL Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis B 9.14 pIC50 0.72 nM IC50 J Med Chem (2016) 59: 8381-8397 [PMID:27556704]
ChEMBL Antagonist activity against Opioid receptor delta 1 in mouse vas deferens assay F 9.2 pA2 9.2 nM pA2 J. Med. Chem. (1997) 40: 3100-3108 [PMID:9301674]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
GtoPdb - - 10.43 pKd 0.04 nM Kd Life Sci (1992) 50: PL119-24 [PMID:1313133]
ChEMBL Displacement of [3H]DADLE from morphine-sensitive Opioid receptor delta 1 (presence of 300 nM DELT-II) of rat brain membranes B 7.91 pKi 12.3 nM Ki J. Med. Chem. (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL Displacement of [3H]DPDPE from DOR in rat brain membranes incubated for 45 mins by liquid scintillation counting B 8.95 pKi 1.13 nM Ki Eur J Med Chem (2019) 168: 189-198 [PMID:30822708]
ChEMBL Binding affinity at delta opioid receptor 1 in rat brain membrane by [3H]DADLE displacement. B 9.09 pKi 0.81 nM Ki J. Med. Chem. (2002) 45: 5378-5383 [PMID:12431065]
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 9.39 pKi 0.41 nM Ki J. Med. Chem. (1999) 42: 3527-3538 [PMID:10479286]
ChEMBL Binding affinity to delta opioid receptor was measured using [3H]DADLE B 9.39 pKi 0.41 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 529-532 [PMID:12565965]
ChEMBL Compound was evaluated for the binding affinity towards Opioid receptor delta 1 in rat brain homogenates using [3H]naltrindole as radioligand B 9.48 pKi 0.33 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 151-156
ChEMBL Displacement of [3H]DADLE from delta opioid receptor in rat cerebrum membranes B 9.54 pKi 0.29 nM Ki Bioorg. Med. Chem. (2012) 20: 949-961 [PMID:22197670]
ChEMBL Displacement of [3H]DADLE from Opioid receptor delta 1 of rat brain membranes (DAMGO quenching mu receptor) B 9.54 pKi 0.29 nM Ki J. Med. Chem. (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL Displacement of [3H]DADLE from delta opioid receptor in rat cerebellum membrane B 9.54 pKi 0.29 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Displacement of [3H]DADLE from morphine-insensitive Opioid receptor delta 1 (presence of 50 nM morphine) of rat brain membranes B 9.62 pKi 0.24 nM Ki J. Med. Chem. (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL Ability to displace [3H]DADLE radioligand from Opioid receptor delta 1 B 9.66 pKi 0.22 nM Ki J. Med. Chem. (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL Ability to displace [3H]DADL from delta opioid receptor B 9.66 pKi 0.22 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL Binding affinity to delta opioid receptor in rat brain membrane B 9.66 pKi 0.22 nM Ki Eur. J. Med. Chem. (2008) 43: 2307-2315 [PMID:18403056]
ChEMBL Binding affinity against Opioid receptor delta 1 from rat brain membranes using [3H]DADLE B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2005) 48: 1620-1629 [PMID:15743203]
ChEMBL Compound was tested for its ability to displace [3H]DADLE from delta receptor in rat brain. B 9.66 pKi 0.22 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 799-804 [PMID:9871544]
ChEMBL Displacement of [3H]p-Cl-DPDPE from rat delta opioid receptor expressed in rat C6 cells B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL Tested for binding affinity against delta opioid receptor by displacing [3H]- DSLET radioligand from rat brain membrane preparations B 9.74 pKi 0.18 nM Ki J. Med. Chem. (1993) 36: 3182-3187 [PMID:8230106]
ChEMBL Compound was evaluated for the binding affinity towards Opioid receptor delta 1 in rat brain homogenates using [3H]DIDI as radioligand B 10.05 pKi 0.09 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 151-156
ChEMBL Ability to inhibit binding of SNC80 to delta opioid receptor B 10.21 pKi 0.06 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL Compound was evaluated for its ability to displace [3H]p-CI-DPDPE in C6 glioma cells expressing the cloned Opioid receptor delta 1 B 10.4 pKi 0.04 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2449-2451 [PMID:11078198]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U50488 from human kappa opioid receptor expressed in CHO cells B 7.12 pKi 75 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL Displacement of [3H]U-69593 from Opioid receptor kappa 1 B 7.52 pKi 30 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2883-2885 [PMID:11597422]
ChEMBL Displacement of [3H]U-69,593 from human KOR expressed in CHO cells B 7.83 pKi 14.7 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL Binding affinity towards recombinant human Opioid receptor kappa 1 transfected in to CHO cells for the displacement of [3H]U-69593 B 8 pKi 10.1 nM Ki J. Med. Chem. (2002) 45: 537-540 [PMID:11784158]
ChEMBL Displacement of [3H]U-69593 from human recombinant kappa opioid receptor expressed in CHO cells B 8 pKi 10.1 nM Ki J. Med. Chem. (2004) 47: 6645-6648 [PMID:15588100]
ChEMBL Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells B 8 pKi 10.1 nM Ki J. Med. Chem. (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. B 8 pKi 10.1 nM Ki J. Med. Chem. (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Binding affinity in recombinant human Opioid receptor kappa 1 transfected into chinese hamster ovary cells by displacing [3H]U-69593 radioligand B 8 pKi 10.1 nM Ki J. Med. Chem. (2003) 46: 3174-3177 [PMID:12825957]
ChEMBL Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method B 8 pKi 10.1 nM Ki Bioorg. Med. Chem. (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL Binding affinity against opioid receptor kappa 1 from human cloned receptor B 8.36 pKi 4.4 nM Ki J. Med. Chem. (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 8.54 pKi 2.9 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL Agonistic activity towards Opioid receptor kappa 1 F 8.31 pEC50 4.95 nM EC50 J. Med. Chem. (2003) 46: 3174-3177 [PMID:12825957]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL Binding affinity against Opioid receptor kappa 1 binding in ICR mouse brain membranes using the radioligand [3H]U-69593 B 6.45 pKi 355 nM Ki J. Med. Chem. (1997) 40: 1977-1981 [PMID:9207938]
ChEMBL Binding affinity against Opioid receptor kappa 1 using [3H]-U-69,593 as radioligand B 8.02 pKi 9.5 nM Ki J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells B 7.38 pKi 42 nM Ki J. Med. Chem. (2001) 44: 857-862 [PMID:11300867]
ChEMBL Binding affinity to kappa opioid receptor in rat brain membrane B 7.52 pKi 30 nM Ki Eur. J. Med. Chem. (2008) 43: 2307-2315 [PMID:18403056]
ChEMBL Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells B 7.59 pKi 25.5 nM Ki J. Med. Chem. (2001) 44: 857-862 [PMID:11300867]
ChEMBL Compound was evaluated for the binding affinity towards Opioid receptor kappa 1 in rat brain homogenates using [3H]CI977 as radioligand B 7.85 pKi 14 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 151-156
ChEMBL Compound was evaluated for its ability to displace [3H]U-69593 in CHO cells expressing the cloned Opioid receptor kappa 1 B 8.24 pKi 5.8 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2449-2451 [PMID:11078198]
ChEMBL Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells B 8.91 pKi 1.23 nM Ki J. Med. Chem. (2001) 44: 857-862 [PMID:11300867]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes B 6.48 pKi 332 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 B 6.48 pKi 332 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 1 B 6.48 pKi 332 nM Ki J. Med. Chem. (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL The opioid receptor affinity(Ki) was evaluated by competition with 9 (Opioid receptor kappa 1) on guinea pig brain membranes B 6.48 pKi 332 nM Ki J. Med. Chem. (1995) 38: 402-407 [PMID:7853332]
ChEMBL The compound was evaluated for binding affinity against the opioid receptor kappa in guinea pig brain membranes using [3H]- U-69,593 B 6.48 pKi 332 nM Ki J. Med. Chem. (1992) 35: 4325-4329 [PMID:1333013]
ChEMBL Binding affinity against kappa-opioid receptor in guinea pig brain membranes B 6.48 pKi 332 nM Ki J. Med. Chem. (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes B 7.12 pKi 75 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
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 7.45 pKi 35.8 nM Ki J. Med. Chem. (1999) 42: 3527-3538 [PMID:10479286]
ChEMBL Binding affinity for kappa opioid receptor was measured using [3H]U-69593 B 7.45 pKi 35.8 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 529-532 [PMID:12565965]
ChEMBL Displacement of [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain membranes (pretreated with BIT and FIT to block mu and delta sites) B 7.47 pKi 34.1 nM Ki J. Med. Chem. (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL Binding affinity to guinea pig kappa opioid receptor B 7.52 pKi 30.4 nM Ki J. Med. Chem. (2008) 51: 4404-4411 [PMID:18637671]
ChEMBL Ability to displace [3H]U-69593 from kappa opioid receptor B 7.52 pKi 30.4 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL Compound was tested for its ability to displace [3H]U-69593 from kappa receptor in guinea pig brain. B 7.52 pKi 30.4 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 799-804 [PMID:9871544]
ChEMBL Ability to displace [3H]U-69593 radioligand from Opioid receptor kappa 1 B 7.52 pKi 30.4 nM Ki J. Med. Chem. (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL Binding affinity against Opioid receptor kappa 1 from guinea pig brain membranes using [3H]U-69593 B 7.57 pKi 26.92 nM Ki J. Med. Chem. (2005) 48: 1620-1629 [PMID:15743203]
ChEMBL Displacement of [125I]OXY from Opioid receptor kappa 2b of guinea pig brain membranes (pretreated with BIT(mu) and FIT(delta) and in the presence of (-)U50,488) B 7.7 pKi 19.9 nM Ki J. Med. Chem. (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL Binding affinity at kappa opioid receptor 1 in guinea pig brain by [3H]U-69593 displacement. B 7.8 pKi 15.8 nM Ki J. Med. Chem. (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes B 7.83 pKi 14.9 nM Ki J. Med. Chem. (2007) 50: 2144-2156 [PMID:17402725]
ChEMBL Binding affinity to Opioid receptor kappa 1 by using [3H]U-69593 as a radioligand from guinea pig B 7.84 pKi 14.3 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 939-943 [PMID:11294396]
ChEMBL Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum B 7.85 pKi 14.01 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Tested for binding activity against kappa opioid receptor using [3H]U-69593 ligand B 7.85 pKi 14 nM Ki J. Med. Chem. (1994) 37: 579-585 [PMID:8126697]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebrum membranes B 7.85 pKi 14 nM Ki Bioorg. Med. Chem. (2012) 20: 949-961 [PMID:22197670]
ChEMBL Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig B 7.99 pKi 10.2 nM Ki J. Med. Chem. (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum B 8.04 pKi 9.04 nM Ki Bioorg. Med. Chem. (2012) 20: 5810-5831 [PMID:22967810]
ChEMBL The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by U69,593 (Opioid receptor kappa 1) antagonist F 8.05 pKi 8.9 nM Ki J. Med. Chem. (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL Ability to inhibit GTP-gamma-S binding to Opioid receptor kappa 1 of guinea pig caudate. B 8.05 pKi 8.85 nM Ki J. Med. Chem. (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL Ability to inhibit binding of U-69,593 to kappa opioid receptor B 8.05 pKi 8.85 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL Apparent binding affinity of compound was determined by antagonism towards Opioid receptor kappa 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate F 8.06 pKi 8.8 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL Displacement of [3H]DAMGO from kappa opioid receptor in Hartley guinea pig brain membrane B 8.13 pKi 7.44 nM Ki J. Med. Chem. (2008) 51: 4404-4411 [PMID:18637671]
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 8.22 pKi 6 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 529-532 [PMID:12565965]
ChEMBL Antagonist activity against kappa-opioid receptor in guinea pig ileum in the presence of ethylketazocine F 5.7 pIC50 2000 nM IC50 J. Med. Chem. (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane B 7 pIC50 100 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]DAMGO from human mu opioid receptor expressed in CHO cells B 6.82 pKi 151 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL Displacement of [3H]DAMGO from human MOR expressed in CHO cells B 7.51 pKi 30.7 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL Displacement of [3H]DAMGO from Opioid receptor mu 1 B 7.57 pKi 27 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2883-2885 [PMID:11597422]
ChEMBL Tested for binding activity against mu opioid receptor using [3H]DAMGO ligand B 7.84 pKi 14.4 nM Ki J. Med. Chem. (1994) 37: 579-585 [PMID:8126697]
ChEMBL Binding affinity determined against Opioid receptor mu 1 from human cloned receptor B 8.14 pKi 7.2 nM Ki J. Med. Chem. (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Binding affinity towards recombinant human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]DAMGO (mu) B 8.2 pKi 6.3 nM Ki J. Med. Chem. (2002) 45: 537-540 [PMID:11784158]
ChEMBL Inhibition of [3H]DAMGO binding to human Mu opioid receptor expressed in CHO cells B 8.2 pKi 6.3 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 cells B 8.2 pKi 6.3 nM Ki J. Med. Chem. (2004) 47: 6645-6648 [PMID:15588100]
ChEMBL Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. B 8.2 pKi 6.3 nM Ki J. Med. Chem. (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Bioorg. Med. Chem. (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL Binding affinity for human Opioid receptor mu 1 transfected into chinese hamster ovary cells by displacing [3H]DAMGO radioligand