U69593 [Ligand Id: 1655] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL440765 (U-69593) |
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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 | 4.7 | pIC50 | 19952.62 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
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]
