U69593 [Ligand Id: 1655] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL440765 (U-69593)
  • 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 in Mouse [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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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 Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI F 5.7 pKd 1980 nM Kd Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI F 5.7 pKd 1980 nM Kd Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting B 4.9 pKi 12540 nM Ki Eur J Med Chem (2012) 50: 44-54 [PMID:22341895]
ChEMBL Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting B 4.9 pKi 12540 nM Ki Eur J Med Chem (2013) 67: 335-343 [PMID:23880358]
ChEMBL Displacement of [3H]DADLE from human recombinant opioid delta receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method B 4.92 pKi >12000 nM Ki Eur J Med Chem (2015) 92: 531-539 [PMID:25599950]
ChEMBL Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis B 4.92 pKi >12000 nM Ki Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710]
ChEMBL Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting B 5 pKi >10000 nM Ki J Med Chem (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Displacement of [3H]pCl-DPDPE from human delta opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain B 5.87 pKi 1358 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
ChEMBL Binding affinity determined against Opioid receptor delta 1 from human cloned receptor B 6 pKi >1000 nM Ki J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Binding affinity towards Opioid receptor delta 1 by the displacement of [125I]-Deltorphin B 5.23 pIC50 5844 nM IC50 Bioorg Med Chem Lett (2002) 12: 197-200 [PMID:11755353]
ChEMBL Inhibition of [125I]deltorphin binding to human delta opioid receptor from membranes of HEK293 cells B 5.24 pIC50 5800 nM IC50 Bioorg Med Chem Lett (2003) 13: 1141-1145 [PMID:12643930]
ChEMBL Tested for inhibitory concentration against [3H]DPDPE binding at sites of delta-opioid receptor in guinea pig brain membrane B 5.3 pIC50 5000 nM IC50 J Med Chem (1994) 37: 2856-2864 [PMID:8071934]
ChEMBL Inhibitory concentration was determined against delta-opioid receptor using [3H]- DPDPE radioligand B 5.3 pIC50 4970 nM IC50 J Med Chem (1995) 38: 570-579 [PMID:7853350]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. F 5 pEC50 >10000 nM EC50 J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of [3H]DPDPE from mouse whole brain DOR B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum B 6 pKi >1000 nM Ki ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes without cerebellum after 1 hr by liquid scintillation counting analysis B 6.41 pKi 391 nM Ki Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane B 5.3 pKi >5000 nM Ki J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U69,593 from human recombinant opioid kappa receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method B 8.46 pKi 3.5 nM Ki Eur J Med Chem (2015) 92: 531-539 [PMID:25599950]
ChEMBL Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis B 8.46 pKi 3.5 nM Ki Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710]
ChEMBL Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting B 8.46 pKi 3.5 nM Ki Eur J Med Chem (2012) 50: 44-54 [PMID:22341895]
ChEMBL Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting B 8.46 pKi 3.5 nM Ki Eur J Med Chem (2013) 67: 335-343 [PMID:23880358]
ChEMBL Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting B 8.8 pKi 1.6 nM Ki J Med Chem (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Binding affinity towards Wild-type kappa opioid receptor expressed in HEK cells B 8.85 pKi 1.4 nM Ki J Med Chem (2000) 43: 1251-1252 [PMID:10753461]
ChEMBL Binding affinity against opioid receptor kappa 1 from human cloned receptor B 8.95 pKi 1.11 nM Ki J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of [3H]U69593 from human KOR expressed in CHO cells B 8.96 pKi 1.1 nM Ki Bioorg Med Chem Lett (2017) 27: 666-669 [PMID:28011222]
ChEMBL Displacement of [3H]U69,593 from human kappa opioid receptor transfected in CHO cell membranes after 60 mins B 8.98 pKi 1.05 nM Ki Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054]
ChEMBL Binding affinity to kappa opioid receptor B 9.32 pKi 0.47 nM Ki Bioorg Med Chem (2010) 18: 4446-4452 [PMID:20478711]
GtoPdb - - 9.5 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407];
Eur J Pharmacol (1985) 109: 281-4 [PMID:2986999]
ChEMBL Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting B 9.52 pKi 0.3 nM Ki J Med Chem (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. B 9.52 pKi 0.3 nM Ki J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Displacement of [3H]naloxone from kappa opioid receptor expressed in HEK293 cell membrane B 8.1 pIC50 8 nM IC50 J Nat Prod (2010) 73: 988-991 [PMID:20426456]
ChEMBL Binding affinity towards Opioid receptor kappa 1 by the displacement of [125I]-(D-Pro10)-Dynorphin A B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2002) 12: 197-200 [PMID:11755353]
ChEMBL Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cells B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2003) 13: 1141-1145 [PMID:12643930]
ChEMBL Agonist activity at human kappa opioid receptor by [35S]GTPgammaS binding assay F 6.48 pEC50 330 nM EC50 Bioorg Med Chem Lett (2007) 17: 6111-6115 [PMID:17904842]
ChEMBL Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay F 6.68 pEC50 207 nM EC50 J Med Chem (2007) 50: 3596-3603 [PMID:17580847]
ChEMBL Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding F 6.68 pEC50 207 nM EC50 J Nat Prod (2006) 69: 107-112 [PMID:16441078]
ChEMBL Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 20 mins by Hoechst staining-based assay B 6.69 pEC50 205 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay B 6.88 pEC50 131 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay F 7.08 pEC50 83.76 nM EC50 Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839]
ChEMBL Agonist activity at recombinant kappa-opioid receptor in human HEK293 cells by [35S]-GTP-gammaS binding assay F 7.1 pEC50 80 nM EC50 Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182]
ChEMBL Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay F 7.1 pEC50 80 nM EC50 J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL Stimulation of [35S]GTP-gamma-S binding at kappa opioid receptor in human brain cortical membrane F 7.19 pEC50 64.3 nM EC50 Bioorg Med Chem Lett (2006) 16: 3609-3613 [PMID:16650985]
ChEMBL Agonist activity at human kappa opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis F 7.22 pEC50 60.14 nM EC50 Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054]
ChEMBL Agonist activity at human KOR expressed in CHO cells assessed as induction of beta-arrestin-2 recruitment by enzyme fragment complementation assay F 7.28 pEC50 52 nM EC50 Bioorg Med Chem Lett (2018) 28: 2770-2772 [PMID:29426768]
ChEMBL Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay F 7.55 pEC50 28.1 nM EC50 Bioorg Med Chem (2015) 23: 6271-6279 [PMID:26346669]
ChEMBL Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay F 7.55 pEC50 28.1 nM EC50 Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250]
ChEMBL Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 7.55 pEC50 28.1 nM EC50 Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554]
ChEMBL Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. B 7.58 pEC50 26.1 nM EC50 J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay F 7.58 pEC50 26.1 nM EC50 J Med Chem (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis F 7.9 pEC50 12.5 nM EC50 Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684]
ChEMBL Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding F 7.92 pEC50 12 nM EC50 ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605]
ChEMBL Agonist activity at human kappa opioid receptor expressed in HEK-293 cells assessed as stimulation of [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting analysis F 7.92 pEC50 12 nM EC50 J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Agonist activity at human kappa opioid receptor expressed in HEK-293 cells after 45 mins by [35S]GTP-gamma-S binding assay in presence of 10 uM of GDP B 7.92 pEC50 12 nM EC50 Medchemcomm (2016) 7: 317-326
ChEMBL Agonist activity at KOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay F 7.92 pEC50 11.9 nM EC50 J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL Agonist activity at KOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay F 7.93 pEC50 11.75 nM EC50 J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL Agonist activity at human kappa opioid receptor in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding F 7.96 pEC50 11 nM EC50 J Med Chem (2008) 51: 4404-4411 [PMID:18637671]
ChEMBL Agonist activity at human KOR expressed in CHO cells by [35S]GTPgammaS binding assay F 8.1 pEC50 8.03 nM EC50 Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680]
ChEMBL Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay F 8.18 pEC50 6.6 nM EC50 J Nat Prod (2006) 69: 107-112 [PMID:16441078]
ChEMBL Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis B 8.27 pEC50 5.4 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay F 8.28 pEC50 5.3 nM EC50 J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
ChEMBL Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay F 8.59 pEC50 2.6 nM EC50 Bioorg Med Chem Lett (2018) 28: 2770-2772 [PMID:29426768]
ChEMBL Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux F 8.65 pEC50 2.25 nM EC50 Bioorg Med Chem Lett (2007) 17: 6111-6115 [PMID:17904842]
ChEMBL Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay F 9.1 pEC50 0.8 nM EC50 J Med Chem (2014) 57: 10464-10475 [PMID:25426797]
κ receptor in Mouse [GtoPdb: 318] [UniProtKB: P33534]
GtoPdb - - 8.6 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Binding affinity to rat kappa opioid receptor expressed in HEK293 cell membranes B 9 pKd 1 nM Kd Bioorg Med Chem (2015) 23: 3948-3956 [PMID:25593096]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay B 8.24 pKi 5.7 nM Ki ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in rat brain after 60 mins by liquid scintillation counting method B 8.4 pKi 3.98 nM Ki Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512]
ChEMBL Binding constant against E203Q,D204N,D206N,E209Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells B 8.52 pKi 3 nM Ki J Med Chem (2000) 43: 1251-1252 [PMID:10753461]
ChEMBL Binding constant against E203Q,D204N,D206N EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells B 8.62 pKi 2.4 nM Ki J Med Chem (2000) 43: 1251-1252 [PMID:10753461]
ChEMBL Binding constant against D216N,D217N,E218Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells B 8.7 pKi 2 nM Ki J Med Chem (2000) 43: 1251-1252 [PMID:10753461]
GtoPdb - - 8.7 pKi - - - Biochem J (1993) 295 ( Pt 3): 625-8 [PMID:8240267];
Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341]
ChEMBL Binding constant against wild type EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells B 8.85 pKi 1.4 nM Ki J Med Chem (2000) 43: 1251-1252 [PMID:10753461]
ChEMBL Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593 B 9.2 pIC50 0.63 nM IC50 Bioorg Med Chem Lett (1998) 8: 2027-2032 [PMID:9873480]
ChEMBL Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 8.11 pEC50 7.7 nM EC50 ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI F 5.31 pKd 4894 nM Kd Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI F 5.31 pKd 4894 nM Kd Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Binding affinity at Opioid receptor kappa 1 in guinea pig brain membrane determined by using [3H]U-69593 as radioligand B 8.37 pKd 4.3 nM Kd J Med Chem (1988) 31: 2015-2021 [PMID:2845084]
ChEMBL Binding affinity for the Opioid receptor kappa 1 B 8.14 pKi 7.3 nM Ki J Med Chem (1988) 31: 831-836 [PMID:2832603]
ChEMBL Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes B 8.32 pKi 4.8 nM Ki J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig B 8.72 pKi 1.89 nM Ki J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Binding affinity against Opioid receptor kappa 1 in guinea pig. B 8.75 pKi 1.78 nM Ki J Med Chem (1996) 39: 860-872 [PMID:8632410]
ChEMBL Displacement of [3H]U-69593 from guinea pig cerebellum KOR B 8.86 pKi 1.37 nM Ki Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum B 8.86 pKi 1.37 nM Ki ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum after 1 hr by liquid scintillation counting analysis B 8.86 pKi 1.37 nM Ki Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250]
ChEMBL Tested for inhibitory effect on binding of [3H]bremazocine to opioid receptor kappa in guinea pig cerebellum membranes B 8.97 pKi 1.06 nM Ki J Med Chem (1992) 35: 4638-4639 [PMID:1361580]
ChEMBL Displacement of [3H]U-69,593 from KOR in guinea pig brain membranes after 120 mins by scintillation counting method B 9.01 pKi 0.97 nM Ki J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting B 9.01 pKi 0.97 nM Ki J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis B 9.01 pKi 0.97 nM Ki J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Displacement of [3H]U-69,593 from kappa-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting B 9.01 pKi 0.97 nM Ki J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 9.01 pKi 0.97 nM Ki Medchemcomm (2016) 7: 2368-2380
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membarnes by liquid scintillation counting method B 9.01 pKi 0.97 nM Ki Medchemcomm (2016) 7: 317-326
ChEMBL Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane B 9.06 pKi 0.88 nM Ki Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182]
ChEMBL Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain B 9.15 pKi 0.7 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
ChEMBL Tested for inhibitory concentration against [3H]U-69593 binding at sites of kappa-opioid receptor in guinea pig brain membrane B 8.68 pIC50 2.1 nM IC50 J Med Chem (1994) 37: 2856-2864 [PMID:8071934]
ChEMBL Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand B 8.68 pIC50 2.1 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 Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting B 5 pKi >10000 nM Ki J Med Chem (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting B 5.63 pKi 2370 nM Ki Eur J Med Chem (2013) 67: 335-343 [PMID:23880358]
ChEMBL Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting B 5.63 pKi 2370 nM Ki Eur J Med Chem (2012) 50: 44-54 [PMID:22341895]
ChEMBL Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis B 5.7 pKi >2000 nM Ki Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710]
ChEMBL Displacement of [3H]DAMGO from human recombinant opioid mu receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method B 5.7 pKi >2000 nM Ki Eur J Med Chem (2015) 92: 531-539 [PMID:25599950]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting B 5.94 pKi 1145 nM Ki J Med Chem (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. B 5.94 pKi 1145 nM Ki J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Binding affinity determined against Opioid receptor mu 1 from human cloned receptor B 6 pKi >1000 nM Ki J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Inhibition of [125I]Enkephalin binding to human mu opioid receptor from membranes of HEK293 cells B 6.6 pIC50 250 nM IC50 Bioorg Med Chem Lett (2003) 13: 1141-1145 [PMID:12643930]
ChEMBL Binding affinity towards Opioid receptor mu 1 by the displacement of [125I]Enkephalin; Not determined B 6.61 pIC50 248 nM IC50 Bioorg Med Chem Lett (2002) 12: 197-200 [PMID:11755353]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells F 5 pEC50 >10000 nM EC50 J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Displacement of [3H]DAMGO from mouse whole brain MOR B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum B 6 pKi >1000 nM Ki ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes without cerebellum after 1 hr by liquid scintillation counting analysis B 6.26 pKi 548 nM Ki Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250]
ChEMBL Binding affinity against opioid receptor by displacing radioligand [3HlU69,593 B 8.93 pKi 1.18 nM Ki J Med Chem (1994) 37: 3408-3418 [PMID:7932569]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane B 5.14 pKi 7250 nM Ki J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAP F 5.67 pKd 2142 nM Kd Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAP F 5.67 pKd 2142 nM Kd Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition F 6.16 pKd 684 nM Kd Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition F 6.16 pKd 684 nM Kd Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig B 5.73 pKi 1880 nM Ki J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain B 6.16 pKi 692 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
ChEMBL Tested for inhibitory effect on binding of [3H]DAMGO to opioid receptor mu in guinea pig cerebellum membranes B 6.26 pKi 551 nM Ki J Med Chem (1992) 35: 4638-4639 [PMID:1361580]
ChEMBL Binding affinity for the Opioid receptor mu 1 B 7.28 pKi 52 nM Ki J Med Chem (1988) 31: 831-836 [PMID:2832603]
ChEMBL Tested for inhibitory concentration against [3H]DAMGO binding at sites of mu-opioid receptor in guinea pig brain membrane B 5.75 pIC50 1760 nM IC50 J Med Chem (1994) 37: 2856-2864 [PMID:8071934]
ChEMBL Inhibitory concentration was determined against Opioid receptor mu 1 using [3H]- DAMGO radioligand B 5.75 pIC50 1760 nM IC50 J Med Chem (1995) 38: 570-579 [PMID:7853350]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting B 5 pKi >10000 nM Ki J Med Chem (2011) 54: 6531-6537 [PMID:21866885]
Nociceptin receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5492] [UniProtKB: P47748]
ChEMBL Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain B 5.96 pKi 1099 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F