U50488 [Ligand Id: 1652] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL441765 (U-50488) |
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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 | Compound was evaluated for the binding affinity to delta opioid receptor | B | 4.68 | pKi | 21000 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
| ChEMBL | Binding affinity against opioid receptor delta from guinea pig brain membranes using [3H]DADLE as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 2243-2247 [PMID:1319495] |
| ChEMBL | Compound was evaluated for its binding affinity against opioid receptor delta subtype in guinea pig brain (minus cerebellum) using [3H]-DADLE as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1991) 34: 397-403 [PMID:1846921] |
| ChEMBL | Receptor binding affinity towards opioid receptor delta | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 2970-2978 [PMID:1323679] |
| 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 | Affinity for opioid receptor delta sites | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1991) 34: 2624-2633 [PMID:1652025] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 in guinea pig brain membranes using [3H]naltrindole as radioligand | B | 5.6 | pKi | 2500 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2735-2740 [PMID:11591513] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 by displacing the radioligand [3H]naltrindole from guinea pig brain membrane | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (2000) 43: 114-122 [PMID:10633042] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from mouse delta opioid receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| ChEMBL | Binding affinity to mouse DOPR expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| 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] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Tested for binding affinity by [3H]diprenorphine displacement for Opioid receptor delta 1 are carried on crude membrane fractions obtained from the whole rat brain minus cerebellum. | B | 5.09 | pKi | 8100 | nM | Ki | J Med Chem (2000) 43: 2992-3004 [PMID:10956208] |
| ChEMBL | Displacement of [3H]DPDPE from Sprague-Dawley rat delta opioid receptor by liquid scintillation counting | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine human kappa opioid receptor expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method | B | 6.92 | pKi | 120 | nM | Ki | ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376] |
| ChEMBL | Displacement of [3H]-diprenorphine from human KOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method | B | 7.51 | pKi | 31.2 | nM | Ki | J Med Chem (2020) 63: 2673-2687 [PMID:31834798] |
| ChEMBL | Displacement of [3H]-diprenorphine from human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method | B | 7.62 | pKi | 23.9 | nM | Ki | ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778] |
| ChEMBL | Compound was evaluated for the binding affinity to kappa opioid receptor | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
| ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting analysis | B | 8.22 | pKi | 6.08 | nM | Ki | Bioorg Med Chem (2016) 24: 2964-2970 [PMID:27185012] |
| ChEMBL | Displacement of [3H]diprenorphine from human KOPR expressed in CHO cells | B | 8.35 | pKi | 4.5 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1023-1026 [PMID:22204910] |
| ChEMBL | Displacement of [3H]U69593 from human kappa opioid receptor expressed in HEK293 cells by scintillation counting | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2014) 57: 6861-6866 [PMID:25051243] |
| ChEMBL | Displacement of [3H]U69,593 from human KOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
| ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
| ChEMBL | Displacement of [3H]U69,593 from human KOR expressed in HEK293 cells after 90 mins by liquid scintillation counting | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2012) 55: 10292-10296 [PMID:22995061] |
| ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| ChEMBL | Displacement of radiolabeled U50488 from human kappa-type opioid receptor | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]diprenorphine from human KOPR expressed in CHO cells | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2010) 53: 4212-4222 [PMID:20441176] |
| ChEMBL | Inhibition of [3H]diprenorphine binding to human Opioid receptor kappa 1 expressed in chinese hamster ovary cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2761-2765 [PMID:15869877] |
| ChEMBL | Displacement of [3H]diprenorphine binding from human kappa opioid receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5498-5502 [PMID:16945525] |
| ChEMBL | Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4679-4685 [PMID:16777411] |
| ChEMBL | Binding affinity for 1 uM [3H]diprenorphine against human Opioid receptor kappa expressed in chinese hamster ovary cells (CHO cells) | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4169-4173 [PMID:16051487] |
| ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5749-5752 [PMID:20801035] |
| ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method | B | 9.04 | pKi | 0.91 | nM | Ki | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
| ChEMBL | Binding affinity to kappa opioid receptor | B | 9.16 | pKi | 0.69 | nM | Ki | Bioorg Med Chem (2010) 18: 4446-4452 [PMID:20478711] |
| ChEMBL | Binding affinity to human kappa-type opioid receptor by radioligand displacement assay | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| 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 | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
J Pharmacol Exp Ther (2004) 308: 1197-203 [PMID:14718611]; 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]; NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; J Pharmacol Exp Ther (1983) 224: 7-12 [PMID:6129321]; Life Sci (1995) 56: PL201-PL207 [PMID:7869844]; J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330] |
| ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in U2OS cells by radioligand binding assay | B | 10 | pKi | 0.1 | nM | Ki | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in U2OS cells by radioligand binding assay | B | 10.03 | pKi | 0.09 | nM | Ki | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Opioid receptor kappa agonist potency was determined in vitro using rabbit vas deferens(LVD) preparation | F | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (1992) 35: 490-501 [PMID:1310743] |
| ChEMBL | In vitro agonist activity at kappa opioid receptor in rabbit vas deferens. | F | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (1993) 36: 2075-2083 [PMID:8393489] |
| ChEMBL | Displacement of radiolabeled U50488 from human kappa-type opioid receptor | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]dynorphin from human kappa opioid receptor expressed in C6 giloma cells | B | 8.7 | pIC50 | 1.99 | nM | IC50 | Bioorg Med Chem (2009) 17: 5782-5790 [PMID:19640720] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation after 15 mins by EIA | F | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
| ChEMBL | Agonist activity at human KOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay | F | 9.05 | pIC50 | 0.9 | nM | IC50 | Eur J Med Chem (2017) 126: 202-217 [PMID:27776274] |
| ChEMBL | Binding affinity to kappa opioid receptor (unknown origin) by radioligand displacement assay | B | 9.08 | pIC50 | 0.84 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Binding affinity to human kappa-type opioid receptor by radioligand displacement assay | B | 9.12 | pIC50 | 0.75 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay | F | 9.16 | pIC50 | 0.69 | nM | IC50 | J Med Chem (2017) 60: 6733-6750 [PMID:28726402] |
| ChEMBL | Binding activity against human Opioid receptor kappa 1 using [3H]-U 50488 as a radioligand | B | 9.16 | pIC50 | 0.69 | nM | IC50 | J Med Chem (2002) 45: 1395-1398 [PMID:11906279] |
| ChEMBL | Displacement of [3H]U 69593 from human recombinant kappa-opioid receptor expressed in CHO cells measured after 60 mins by scintillation counting method | B | 9.19 | pIC50 | 0.64 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Inhibition of human kappa opioid receptor | B | 9.26 | pIC50 | 0.55 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay | F | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2017) 60: 6733-6750 [PMID:28726402] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem (2014) 22: 4694-4703 [PMID:25087049] |
| ChEMBL | Agonist activity at human KOR expressed in EE-HEK293 cells | B | 6.2 | pEC50 | 630.96 | nM | EC50 | Bioorg Med Chem (2016) 24: 2832-2842 [PMID:27234885] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | F | 7.1 | pEC50 | 80 | nM | EC50 | ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins | F | 7.34 | pEC50 | 46 | nM | EC50 | Bioorg Med Chem (2007) 15: 4106-4112 [PMID:17433695] |
| ChEMBL | Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.34 | pEC50 | 46 | nM | EC50 | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding | F | 7.34 | pEC50 | 46 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1508-1511 [PMID:17276685] |
| ChEMBL | Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined | F | 7.34 | pEC50 | 46 | nM | EC50 | J Med Chem (2003) 46: 5162-5170 [PMID:14613319] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.44 | pEC50 | 36 | nM | EC50 | J Med Chem (2006) 49: 5635-5639 [PMID:16942039] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 2128-2133 [PMID:23434225] |
| ChEMBL | Activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem (2008) 16: 5653-5664 [PMID:18417347] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 365-368 [PMID:19091564] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6516-6520 [PMID:17935988] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7340-7344 [PMID:23142613] |
| ChEMBL | Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in U2OS cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL |
Human Opioid receptor kappa 1 mediated stimulation of [35S]- GTPgammaS binding in CHO cells (Agonist potency). |
B | 7.84 | pEC50 | 14.4 | nM | EC50 | J Med Chem (2000) 43: 2698-2702 [PMID:10893307] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay | F | 7.88 | pEC50 | 13.3 | nM | EC50 | J Med Chem (2020) 63: 2673-2687 [PMID:31834798] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay | F | 8.03 | pEC50 | 9.31 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 8.11 | pEC50 | 7.8 | nM | EC50 | ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding | F | 8.2 | pEC50 | 6.3 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 5749-5752 [PMID:20801035] |
| ChEMBL | Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | F | 8.24 | pEC50 | 5.7 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1023-1026 [PMID:22204910] |
| ChEMBL | Effective concentration for activation of human Opioid receptor kappa 1 expressed in chinese hamster ovary cells to enhance [35S]GTP-gamma-S, binding | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2761-2765 [PMID:15869877] |
| ChEMBL | Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4679-4685 [PMID:16777411] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting | F | 8.38 | pEC50 | 4.2 | nM | EC50 | J Med Chem (2012) 55: 3878-3890 [PMID:22439881] |
| ChEMBL | Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.47 | pEC50 | 3.4 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5498-5502 [PMID:16945525] |
| ChEMBL | Concentration required to enhance [35S]GTP-gamma-S, binding to human Opioid receptor kappa expressed in CHO cells | F | 8.47 | pEC50 | 3.4 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4169-4173 [PMID:16051487] |
| ChEMBL | Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding | F | 8.54 | pEC50 | 2.9 | nM | EC50 | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | F | 8.56 | pEC50 | 2.77 | nM | EC50 | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis | F | 8.74 | pEC50 | 1.8 | nM | EC50 | Bioorg Med Chem (2018) 26: 4254-4263 [PMID:30054192] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2019) 62: 11054-11070 [PMID:31738550] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as binding affinity of U50,488 to orthosteric binding site incubated with U50,488 alone for 90 mins by radioligand competition binding assay | B | 8.09 | pKi | 8.1 | nM | Ki | J Nat Prod (2021) 84: 2238-2248 [PMID:34308635] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 using [3H]U-69593 as a radioligand | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (1991) 34: 1891-1896 [PMID:1648141] |
| ChEMBL | Agonist activity at kappa opioid receptor in ddy mouse vas deferens assessed as inhibition of electric stimulation-induced contraction | F | 8.63 | pIC50 | 2.35 | nM | IC50 | Bioorg Med Chem (2008) 16: 9188-9201 [PMID:18829333] |
| ChEMBL | Agonist activity at mouse FLAG-tagged kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay | F | 8.82 | pIC50 | 1.5 | nM | IC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Agonist activity at mouse FLAG-tagged kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay | F | 8.9 | pIC50 | 1.26 | nM | IC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| GtoPdb | - | - | 9 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575] |
| ChEMBL | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as beta-arrestin recruitment by measuring U50,488 EC50 using furimazine as a substrate pretreated for 5 mins followed by incubation with U50,488 measured for 35 mins by BRET assay | B | 5.31 | pEC50 | 4886 | nM | EC50 | J Nat Prod (2021) 84: 2238-2248 [PMID:34308635] |
| ChEMBL | Agonist activity at mouse cloned kappa opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | F | 7.66 | pEC50 | 21.7 | nM | EC50 | Eur J Med Chem (2013) 69: 786-789 [PMID:24103580] |
| ChEMBL | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as inhibition of forskolin induced cAMP production by measuring U50,488 EC50 incubated with U50,488 alone measured after 30 mins by HTRF assay | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Nat Prod (2021) 84: 2238-2248 [PMID:34308635] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Biochem J (1993) 295 ( Pt 3): 625-8 [PMID:8240267]; Biochem J (1993) 295 ( Pt 3): 629-33 [PMID:8240268]; Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341] |
| ChEMBL | Displacement of [3H]U69593 from rat KOR expressed in CHO cells | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem (2016) 24: 5280-5290 [PMID:27624520] |
| ChEMBL | Displacement of [3H]U 69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting | B | 9.35 | pKi | 0.45 | nM | Ki | J Med Chem (2017) 60: 349-361 [PMID:27997171] |
| ChEMBL | Displacement of [3H]U 69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting | B | 9.17 | pIC50 | 0.68 | nM | IC50 | J Med Chem (2017) 60: 349-361 [PMID:27997171] |
| ChEMBL | Displacement of [3H]U 69593 from rat recombinant kappa-type opioid receptor expressed in CHO cells | B | 9.19 | pIC50 | 0.64 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity towards kappa opioid receptor using [3H]-BREM in guinea pig ileum | B | 5.89 | pKi | 1298 | nM | Ki | J Med Chem (1989) 32: 1996-2002 [PMID:2547074] |
| ChEMBL | Compound was evaluated for binding affinity towards kappa opioid receptor using [3H](-)-U-69,593 in guinea pig ileum | B | 6.52 | pKi | 299 | nM | Ki | J Med Chem (1989) 32: 1996-2002 [PMID:2547074] |
| ChEMBL | Binding affinity for kappa opioid receptor in presence of 120 mM NaCl and 50 micro M Gpp(NH)p | B | 6.69 | pKi | 204 | nM | Ki | J Med Chem (1993) 36: 1860-1865 [PMID:8390575] |
| ChEMBL | Compound was evaluated for binding affinity towards Opioid receptor kappa 1 using [3H]BREM in guinea pig ileum | B | 6.96 | pKi | 109 | nM | Ki | J Med Chem (1989) 32: 1996-2002 [PMID:2547074] |
| ChEMBL | Binding affinity for kappa opioid receptor was evaluated by displacing [3H]- diprenorphine | B | 7.69 | pKi | 20.5 | nM | Ki | J Med Chem (1993) 36: 1860-1865 [PMID:8390575] |
| ChEMBL | Binding affinity for kappa opioid receptor in absence of 120 mM NaCl and 50 micro M Gpp(NH)p | B | 7.78 | pKi | 16.5 | nM | Ki | J Med Chem (1993) 36: 1860-1865 [PMID:8390575] |
| ChEMBL | Binding affinity against opioid receptor kappa from guinea pig brain membranes using [3H]ethylketocyclazocine as radioligand | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1992) 35: 2243-2247 [PMID:1319495] |
| ChEMBL | Binding affinity for the Opioid receptor kappa 1 | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Opioid receptor kappa affinity, determined with [3H]etorphine in the presence of excess unlabeled [D-Ala2-MePhe4-Glyol5]-enkephalin | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1991) 34: 190-194 [PMID:1846919] |
| ChEMBL | Displacement of [3H]-U-69,593 from Opioid receptor kappa 1 in guinea pig cerebellar. | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2000) 43: 2992-3004 [PMID:10956208] |
| ChEMBL | Receptor binding affinity towards opioid receptor kappa | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1992) 35: 2970-2978 [PMID:1323679] |
| ChEMBL | Displacement of [3H]-BRL 52537 from opioid receptor kappa site in guinea pig | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1991) 34: 2624-2633 [PMID:1652025] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 8.78 | pKi | 1.67 | nM | Ki | ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605] |
| ChEMBL | Displacement of [3H]Cl-977 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2014) 57: 6845-6860 [PMID:25062506] |
| ChEMBL | Tested for inhibitory effect on binding of [3H]bremazocine to opioid receptor kappa in guinea pig cerebellum membranes | B | 8.94 | pKi | 1.16 | nM | Ki | J Med Chem (1992) 35: 4638-4639 [PMID:1361580] |
| ChEMBL | Displacement of [3H]U69593 from Sprague-Dawley rat kappa opioid receptor in guinea pig cerebella by liquid scintillation counting | B | 8.94 | pKi | 1.14 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptors in guine pig brain (minus cerebellum). | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (1991) 34: 397-403 [PMID:1846921] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 in guinea pig. | B | 9.04 | pKi | 0.91 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| ChEMBL | Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 in guinea pig brain homogenates | B | 9.05 | pKi | 0.89 | nM | Ki | J Med Chem (2000) 43: 2124-2134 [PMID:10841791] |
| ChEMBL | Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (2001) 44: 2814-2826 [PMID:11495592] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane | B | 9.31 | pKi | 0.49 | nM | Ki | Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073] |
| ChEMBL | Binding affinity towards Opioid receptor kappa 1 by displacing the radioligand [3H]U-69593 from guinea pig brain membrane | B | 9.44 | pKi | 0.36 | nM | Ki | J Med Chem (2000) 43: 114-122 [PMID:10633042] |
| ChEMBL | Binding affinity towards Opioid receptor kappa 1 in guinea pig brain membranes using [3H]U-69593 as radioligand | B | 9.44 | pKi | 0.36 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2735-2740 [PMID:11591513] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2014) 57: 6845-6860 [PMID:25062506] |
| ChEMBL | Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182] |
| ChEMBL | Displacement of [3H]-U69,593 from KOR in guinea pig brain membranes incubated for 30 mins by liquid scintillation counting | B | 9.47 | pKi | 0.34 | nM | Ki | Eur J Med Chem (2019) 168: 189-198 [PMID:30822708] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes after 150 mins by scintillation counting | B | 9.51 | pKi | 0.31 | nM | Ki | Eur J Med Chem (2011) 46: 1972-1982 [PMID:21481987] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting | B | 9.51 | pKi | 0.31 | nM | Ki | J Med Chem (2010) 53: 4212-4222 [PMID:20441176] |
| ChEMBL | Displacement of [3H]-U69,593 from KOR in guinea pig brain membranes incubated for 30 mins by liquid scintillation counting | B | 9.57 | pKi | 0.27 | nM | Ki | ACS Med Chem Lett (2020) 11: 678-685 [PMID:32435370] |
| ChEMBL | Compound was evaluated for the opioid receptor kappa affinity using guinea pig brain membranes. | B | 7.02 | pIC50 | 96 | nM | IC50 | J Med Chem (1991) 34: 181-189 [PMID:1846918] |
| ChEMBL | Binding affinity against opioid receptor kappa, in guinea pig brain membrane, using [3H]bremazocine as the radioligand. | B | 7.02 | pIC50 | 95.5 | nM | IC50 | J Med Chem (1991) 34: 3149-3158 [PMID:1659636] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 8.94 | pIC50 | 1.14 | nM | IC50 | Bioorg Med Chem (2008) 16: 4304-4312 [PMID:18337104] |
| ChEMBL | Agonist activity at kappa opioid receptor in guinea pig ileum assessed as inhibition of electric stimulation-induced contraction | F | 8.95 | pIC50 | 1.12 | nM | IC50 | Bioorg Med Chem (2008) 16: 9188-9201 [PMID:18829333] |
| ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig cerebellum | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6398-6401 [PMID:18990576] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Compound was evaluated for the binding affinity to mu opioid receptor | B | 6.08 | pKi | 825 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 5.32 | pEC50 | 4840 | nM | EC50 | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor mu 1 using [3H]etorphine as a radioligand | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1991) 34: 1891-1896 [PMID:1648141] |
| 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] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Binding affinity for mu opioid receptor was evaluated by displacing [3H]- diprenorphine | B | 5.67 | pKi | 2128 | nM | Ki | J Med Chem (1993) 36: 1860-1865 [PMID:8390575] |
| ChEMBL | Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting | B | 5.76 | pKi | 1750 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Displacement of [3H]diprenorphine from rat mu opioid receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| ChEMBL | Binding affinity to rat MOPR expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Tested for binding affinity by [3H]diprenorphine displacement for Opioid receptor mu 1 was carried on crude membrane fractions obtained from the whole rat brain minus cerebellum.. | B | 6.15 | pKi | 716 | nM | Ki | J Med Chem (2000) 43: 2992-3004 [PMID:10956208] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity for the Opioid receptor mu 1 | B | 6.06 | pKi | 880 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Compound was evaluated for the opioid receptor mu affinity determined with [3H][D-Ala2-MePhe4-Gly-ol5]-enkephalin (DAGOL) in the presence of excess unlabeled DAGOL to suppress mu binding. | B | 6.06 | pKi | 880 | nM | Ki | J Med Chem (1991) 34: 190-194 [PMID:1846919] |
| ChEMBL | Binding affinity against opioid receptor mu from guinea pig brain membranes using [3H]naloxone as radioligand | B | 6.08 | pKi | 825 | nM | Ki | J Med Chem (1992) 35: 2243-2247 [PMID:1319495] |
| ChEMBL | Affinity for opioid receptor mu sites | B | 6.21 | pKi | 616 | nM | Ki | J Med Chem (1991) 34: 2624-2633 [PMID:1652025] |
| ChEMBL | Displacement of [3H]DAGO from mu opioid receptors in guinea pig brain (minus cerebellum). | B | 6.21 | pKi | 616 | nM | Ki | J Med Chem (1991) 34: 397-403 [PMID:1846921] |
| ChEMBL | Receptor binding affinity towards opioid receptor mu | B | 6.21 | pKi | 616 | nM | Ki | J Med Chem (1992) 35: 2970-2978 [PMID:1323679] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 in guinea pig brain membranes using [3H]DAMGO as radioligand | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2735-2740 [PMID:11591513] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from guinea pig brain membrane | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2000) 43: 114-122 [PMID:10633042] |
| ChEMBL | Tested for inhibitory effect on binding of [3H]DAMGO to opioid receptor mu in guinea pig cerebellum membranes | B | 6.69 | pKi | 206 | nM | Ki | J Med Chem (1992) 35: 4638-4639 [PMID:1361580] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity towards sigma opioid receptor using [3H](+)-3-PPP in guinea pig ileum | B | 5.9 | pKi | 1270 | nM | Ki | J Med Chem (1989) 32: 1996-2002 [PMID:2547074] |
| ChEMBL | Compound was evaluated for binding affinity towards sigma opioid receptor using [3H](+)-3-PPP in guinea pig ileum | B | 6.06 | pKi | 874 | nM | Ki | J Med Chem (1989) 32: 1996-2002 [PMID:2547074] |
| ChEMBL | Compound was evaluated for the binding affinity to sigma opioid receptor | B | 6.16 | pKi | 696 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
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]
