morphine [Ligand Id: 1627] activity data from GtoPdb and ChEMBL

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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)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • α2A-adrenoceptor/μ receptor/Mu opioid receptor/Alpha-2A adrenergic receptor in Human [ChEMBL: CHEMBL3883321] [GtoPdb: 25319] [UniProtKB: P08913P35372]
  • α2A-adrenoceptor/μ receptor in Rat [GtoPdb: 25319] [UniProtKB: P22909P33535]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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 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