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ChEMBL ligand: CHEMBL70 (Anhydrous morphine, Avinza, Depodur, Hydromorphone hydrochloride impurity, morphine-, IDS-NM-009, Infumorph, Kadian, Morphia, Morphine, Morphine anhydrous, Morphine (anhydrous), Morphine extended release, Morphine polistirex, Morphium, N02AA01, Nepenthe, Ospalivina) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | Binding affinity against Opioid receptor delta 1 in guinea pig brain membranes | B | 6.15 | pKi | 710 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
ChEMBL | Binding affinities against Opioid receptor delta 1 of guinea pig brain membrane using [3H]DPDPE as the radioligand using competition binding assays. | B | 6.2 | pKi | 629.51 | nM | Ki | J Med Chem (1990) 33: 206-212 [PMID:1967312] |
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 | 6.22 | pKi | 605 | 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 | 6.22 | pKi | 605 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
ChEMBL | Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 6.22 | pKi | 605 | 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 | 6.22 | pKi | 605 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
ChEMBL | Binding affinity against Opioid receptor delta 1 was determined in brain membrane preparations from male Hartley guinea-pigs | B | 6.29 | pKi | 510 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439] |
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 | 6.34 | pKi | 460 | nM | Ki | J Med Chem (1991) 34: 397-403 [PMID:1846921] |
ChEMBL | Affinity for opioid receptor delta sites | B | 6.34 | pKi | 456 | nM | Ki | J Med Chem (1991) 34: 2624-2633 [PMID:1652025] |
ChEMBL | Receptor binding affinity towards opioid receptor delta | B | 6.34 | pKi | 456 | nM | Ki | J Med Chem (1992) 35: 2970-2978 [PMID:1323679] |
ChEMBL | Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig | B | 6.34 | pKi | 456 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
ChEMBL | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor delta 1 using [3H]DPDPE as radioligand | B | 6.38 | pKi | 416.87 | nM | Ki | J Med Chem (2002) 45: 1949-1956 [PMID:11960505] |
ChEMBL | In vivo binding affinity against delta Opioid receptor was measured by using labeled ligand [3H]DADLE (1 nM) with 4 nM sufentanil | B | 6.43 | pKi | 375 | nM | Ki | J Med Chem (1994) 37: 3121-3127 [PMID:7932535] |
ChEMBL | Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes incubated for 1 hr by scintillation counting method | B | 6.47 | pKi | 340 | nM | Ki | Eur J Med Chem (2018) 151: 495-507 [PMID:29649744] |
ChEMBL | Binding affinity determined against Opioid receptor delta 1 from human cloned receptor | B | 6.52 | pKi | 299 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
ChEMBL | Displacement of [3H]DPDPE from delta-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | B | 6.53 | pKi | 295 | nM | Ki | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
ChEMBL | Binding affinity towards Opioid receptor delta 1 | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
ChEMBL | In vitro potency was measured against human Opioid receptor delta 1 | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
ChEMBL | Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor delta 1 expressed in CHO cell membrane;Range is between (63-360) | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
ChEMBL | Binding affinity towards Opioid receptor delta 1 of guinea pig brain membranes using radioligand 0.2 nM [3H]Naltrindole | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1717-1721 [PMID:11425545] |
ChEMBL | Inhibition of [3H]naltrindole binding to opioid receptor delta 1 of Chinese hamster ovary membrane | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2004) 47: 1886-1888 [PMID:15055988] |
ChEMBL | Binding affinity to displace radioligand [3H]naltrindole on Opioid receptor delta 1 in guinea pig membranes. | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2000) 43: 3558-3565 [PMID:11000010] |
ChEMBL | Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2006) 49: 256-262 [PMID:16392810] |
ChEMBL | Displacement of [3H]Cl-DPDPE from human recombinant DOR expressed in CHO cells | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
ChEMBL | Displacement of [3H]DPDPE from human cloned delta opioid receptor | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
ChEMBL | Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2012) 55: 3878-3890 [PMID:22439881] |
ChEMBL | Activity was evaluated by inhibition of the binding of 1 nM [3H]DPDPE at Opioid receptor delta 1 binding site | B | 6.88 | pKi | 132 | nM | Ki | J Med Chem (1996) 39: 1956-1966 [PMID:8642554] |
GtoPdb | - | - | 6.9 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL | Binding affinity for Opioid receptor delta 1 was determined | B | 6.95 | pKi | 113.3 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3141-3143 [PMID:12372519] |
ChEMBL | Displacement of [3H]diprenorphine from recombinant delta opioid receptor expressed in C6 cells | B | 6.98 | pKi | 104.57 | nM | Ki | J Med Chem (2008) 51: 2316-2320 [PMID:18311899] |
ChEMBL | Displacement of [3H]diprenorphine from human DOR expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting assay | B | 6.98 | pKi | 104.1 | nM | Ki | J Med Chem (2020) 63: 1671-1683 [PMID:31986033] |
ChEMBL | Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
ChEMBL | Compound was evaluated for the binding affinity to delta opioid receptor | B | 7.29 | pKi | 51 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
ChEMBL | Binding to delta opioid receptor by using [3H]DPDPE as radioligand in guinea pig brain minus cerebellum | B | 6.37 | pIC50 | 430 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2527-2532 |
ChEMBL | Evaluated for the inhibition of [3H]DADLE binding to Opioid receptor delta 1 of guinea pig brain | B | 6.73 | pIC50 | 185 | nM | IC50 | J Med Chem (1987) 30: 1538-1542 [PMID:2887656] |
ChEMBL | In vitro binding affinity against cloned human Opioid receptor delta 1 expressed in HEK 293S cells | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2003) 46: 34-48 [PMID:12502358] |
ChEMBL | Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | F | 6.11 | pEC50 | 780 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
ChEMBL | Agonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay | F | 6.23 | pEC50 | >593 | nM | EC50 | J Med Chem (2020) 63: 1671-1683 [PMID:31986033] |
ChEMBL | Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.3 | pEC50 | 500 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
ChEMBL | Stimulation of [35S]GTP-gamma-S binding to human recombinant DOR | F | 6.5 | pEC50 | 316 | nM | EC50 | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 6.5 | pEC50 | 316 | nM | EC50 | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins | F | 7.81 | pEC50 | 15.6 | nM | EC50 | J Med Chem (2011) 54: 980-988 [PMID:21235243] |
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
ChEMBL | In vitro agonistic activity against opioid receptor delta of mouse vas deferens | F | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2005) 48: 3372-3378 [PMID:15857143] |
ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6398-6401 [PMID:18990576] |
ChEMBL | Evaluated for inhibitory activity against Opioid receptor delta 1 of mouse vas deferens (MVD). | B | 6.13 | pIC50 | 736 | nM | IC50 | J Med Chem (1990) 33: 206-212 [PMID:1967312] |
ChEMBL | Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor) | F | 6.19 | pIC50 | 644 | nM | IC50 | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in ICR mouse whole brain | B | 6.3 | pIC50 | <500 | nM | IC50 | Bioorg Med Chem (2008) 16: 4304-4312 [PMID:18337104] |
ChEMBL | Inhibitory potency against delta Opioid receptor delta 1 in longitudinal muscle preparation of mouse vas deferens | B | 6.41 | pIC50 | 390 | nM | IC50 | J Med Chem (1981) 24: 1119-1124 [PMID:6276540] |
ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | B | 6.81 | pIC50 | 155 | nM | IC50 | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
ChEMBL | Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
ChEMBL | Binding affinity towards Opioid receptor delta 1 using [3H]DADLE as radioligand. | B | 6.16 | pKi | 684 | nM | Ki | J Med Chem (1995) 38: 1547-1557 [PMID:7739013] |
ChEMBL | Inhibition of [3H]DSLET binding to delta 1 opioid receptors in rat brain membranes | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
ChEMBL | In vitro binding affinity at opioid receptor delta 1 was determined in C6 rat glioma cells using [3H]Ile5,6 deltorphin II | B | 6.66 | pKi | 217 | nM | Ki | J Med Chem (2003) 46: 1758-1763 [PMID:12699394] |
ChEMBL | Inhibition of [3H][Ile5,6]deltorphin II binding to opioid receptor delta from rat brain membranes | B | 6.66 | pKi | 217 | nM | Ki | J Med Chem (2005) 48: 3372-3378 [PMID:15857143] |
ChEMBL | Binding affinity against Opioid receptor delta 1 isolated from rat brain membrane was determined using [3H][Ile]-deltorphin as radioligand | B | 6.66 | pKi | 217 | nM | Ki | J Med Chem (2003) 46: 4182-4187 [PMID:12954070] |
ChEMBL | Displacement of [3H[Ile5,6]-deltorphin II from delta opioid receptor of rat brain membranes | B | 6.66 | pKi | 217 | nM | Ki | J Med Chem (2005) 48: 5052-5055 [PMID:16033285] |
ChEMBL | Displacement of [3H]-diprenorphine from rat delta-type opioid receptor expressed in rat C6 cell membranes incubated for 1 hr by liquid scintillation counting method | B | 6.77 | pKi | 171 | nM | Ki | J Med Chem (2019) 62: 4142-4157 [PMID:30924650] |
ChEMBL | Displacement of [3H]diprenorphine from rat DOR expressed in rat C6 cells after 1 hr by liquid scintillation counting analysis | B | 6.77 | pKi | 171 | nM | Ki | J Med Chem (2013) 56: 2139-2149 [PMID:23419026] |
ChEMBL | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
ChEMBL | Displacement of [3H]DPDPE from rat delta opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method | B | 6.93 | pKi | 116.8 | nM | Ki | J Med Chem (2021) 64: 12414-12433 [PMID:34387468] |
ChEMBL | Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain membrane by liquid scintillation counting | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (2011) 54: 980-988 [PMID:21235243] |
ChEMBL | Inhibition of [3H]DPDPE radioligand binding to rat opioid receptor delta 1 site from rat brain membranes | B | 7.05 | pKi | 90 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1109-1111 [PMID:10843229] |
ChEMBL | Inhibition of binding of [3H]-DPDPE to opioid receptor delta 1 from rat brain membrane. | B | 7.05 | pKi | 90 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1741-1743 [PMID:11425550] |
ChEMBL | Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (2003) 46: 623-633 [PMID:12570383] |
ChEMBL | Displacement of [3H]DSLET from delta opioid receptor in rat brain membranes | B | 7.08 | pKi | 82.5 | nM | Ki | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
ChEMBL | Displacement of [3H]diprenorphine from rat delta receptor expressed in CHO cells by scintillation counting | B | 7.11 | pKi | 76.9 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 418-421 [PMID:19932964] |
ChEMBL | Inhibition of [3H]-[D-Pen2, D-Pen5]-enkephalin (2 nM) to Opioid receptor delta 1 of male Sprague-Dawley rat brain homogenate | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 589-592 |
ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting analysis | B | 8.7 | pKi | 2 | nM | Ki | Medchemcomm (2016) 7: 2368-2380 |
ChEMBL | Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in rat membranes after 120 mins by scintillation counting analysis | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2019) 62: 4204-4217 [PMID:30939014] |
ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in rat brain membranes | B | 8.74 | pKi | 1.8 | nM | Ki | Eur J Med Chem (2011) 46: 1972-1982 [PMID:21481987] |
ChEMBL | Inhibition of [3H]- DADLE binding to Rat brain Opioid receptor delta 1 | B | 6.16 | pIC50 | 684 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
ChEMBL | Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1. | B | 6.16 | pIC50 | 684 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
ChEMBL | Displacement of [3H]deltorphin-2 from delta opioid receptor from Wistar rat brain by liquid scintillation counting | B | 6.39 | pIC50 | 404 | nM | IC50 | Bioorg Med Chem (2010) 18: 3535-3542 [PMID:20413312] |
ChEMBL | Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane | B | 6.69 | pIC50 | 205 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
ChEMBL | Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1. | B | 8.13 | pIC50 | 7.37 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Compound was evaluated for the binding affinity to kappa opioid receptor | B | 5.72 | pKi | 1900 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 6.52 | pKi | 299 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
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 | 6.52 | pKi | 299 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 6.52 | pKi | 299 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
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 | 6.52 | pKi | 299 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
ChEMBL | In vitro potency was measured against human Opioid receptor kappa 1 | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
ChEMBL | Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor kappa 1 expressed in CHO cell membrane | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
ChEMBL | Binding affinity to human kappa opioid receptor | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
ChEMBL | In vitro binding affinity at opioid receptor kappa 1 was determined in human CHO cells using [3H]U-69593 | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (2003) 46: 1758-1763 [PMID:12699394] |
ChEMBL | Binding affinity towards Opioid receptor kappa 1 was determined | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1989) 32: 1620-1626 [PMID:2567782] |
ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method | B | 7.11 | pKi | 76.9 | nM | Ki | J Med Chem (2021) 64: 12414-12433 [PMID:34387468] |
ChEMBL | Displacement of [3H]diprenorphine from recombinant kappa opioid receptor expressed in CHO cells | B | 7.18 | pKi | 65.5 | nM | Ki | J Med Chem (2008) 51: 2316-2320 [PMID:18311899] |
ChEMBL | Binding affinity against opioid receptor kappa 1 from human cloned receptor | B | 7.19 | pKi | 64 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
ChEMBL | Displacement of [3H]-diprenorphine from human kappa-type opioid receptor expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting method | B | 7.21 | pKi | 61 | nM | Ki | J Med Chem (2019) 62: 4142-4157 [PMID:30924650] |
ChEMBL | Displacement of [3H]diprenorphine from human KOR expressed in CHO cells after 1 hr by liquid scintillation counting analysis | B | 7.22 | pKi | 60.9 | nM | Ki | J Med Chem (2013) 56: 2139-2149 [PMID:23419026] |
ChEMBL | Binding affinity for Opioid receptor kappa 1 was determined. | B | 7.28 | pKi | 52.14 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3141-3143 [PMID:12372519] |
GtoPdb | - | - | 7.3 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL | Displacement of [3H]U-69593 from human cloned kappa opioid receptor | B | 7.33 | pKi | 46.9 | nM | Ki | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
ChEMBL | Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cells | B | 7.33 | pKi | 46.9 | nM | Ki | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
ChEMBL | Displacement of [3H]diprenorphine from human KOR expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting assay | B | 7.43 | pKi | 36.8 | nM | Ki | J Med Chem (2020) 63: 1671-1683 [PMID:31986033] |
ChEMBL | Binding affinity to kappa opioid receptor | B | 7.47 | pKi | 33.7 | nM | Ki | Bioorg Med Chem (2010) 18: 4446-4452 [PMID:20478711] |
ChEMBL | Binding affinity towards opioid receptor kappa 2 | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
ChEMBL | Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of Chinese hamster ovary membrane | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2004) 47: 1886-1888 [PMID:15055988] |
ChEMBL | Displacement of [3H]-U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2012) 55: 3878-3890 [PMID:22439881] |
ChEMBL | Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2006) 49: 256-262 [PMID:16392810] |
ChEMBL | Displacement of [3H]diprenorphine from kappa-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
ChEMBL | Displacement of [3H]diprenorphine from human kappa receptor expressed in CHO cells by scintillation counting | B | 8.16 | pKi | 6.9 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 418-421 [PMID:19932964] |
ChEMBL | In vitro binding affinity against cloned human Opioid receptor kappa 1 expressed in HEK 293S cells | B | 5.77 | pIC50 | 1705.1 | nM | IC50 | J Med Chem (2003) 46: 34-48 [PMID:12502358] |
ChEMBL | Stimulation of [35S]GTP-gamma-S binding to human recombinant KOR | F | 6.32 | pEC50 | 484 | nM | EC50 | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 6.32 | pEC50 | 484 | nM | EC50 | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding |