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) |
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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 | F | 6.32 | pEC50 | 484 | nM | EC50 | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins | F | 6.32 | pEC50 | 484 | nM | EC50 | J Med Chem (2011) 54: 980-988 [PMID:21235243] |
| ChEMBL | Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| ChEMBL | Agonist activity at human kappa 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 | 6.48 | pEC50 | 330 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Binding affinities against Opioid receptor kappa 1 of guinea pig brain membrane using [3H]U69,593 as the radioligand using competition binding assays. | B | 5.81 | pKi | 1549.49 | nM | Ki | J Med Chem (1990) 33: 206-212 [PMID:1967312] |
| ChEMBL | Evaluated for the binding affinity at kappa receptor | B | 6.52 | pKi | 301 | nM | Ki | J Med Chem (1994) 37: 3482-3491 [PMID:7932577] |
| ChEMBL | Agonist activity at kappa opioid receptor in ddy mouse vas deferens assessed as inhibition of electric stimulation-induced contraction | F | 6.84 | pIC50 | 145.1 | nM | IC50 | Bioorg Med Chem (2008) 16: 9188-9201 [PMID:18829333] |
| ChEMBL | Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor kappa 1 isolated from rat brain membrane was determined using [3H]U-69593 as radioligand | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (2003) 46: 4182-4187 [PMID:12954070] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor of rat brain membranes | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (2005) 48: 5052-5055 [PMID:16033285] |
| GtoPdb | - | - | 7 | pKi | - | - | - |
Biochem J (1993) 295 ( Pt 3): 625-8 [PMID:8240267]; Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341] |
| ChEMBL | Inhibition of 9 (2 nM) binding to Opioid receptor kappa 1 of rat brain homogenate | B | 7.57 | pKi | 27 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 589-592 |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| ChEMBL | Binding affinity for kappa opioid receptor was evaluated by displacing [3H]- diprenorphine | B | 5.19 | pKi | 6424 | nM | Ki | J Med Chem (1993) 36: 1860-1865 [PMID:8390575] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 was determined in brain membrane preparations from male Hartley guinea-pigs | B | 5.73 | pKi | 1870 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439] |
| ChEMBL | In vivo binding affinity against kappa opioid receptor was measured by using labeled ligand [3H]ethylketocyclazocine (1 nM) with 500 nM DADLE and 20 nM sufentanil | B | 5.73 | pKi | 1870 | nM | Ki | J Med Chem (1994) 37: 3121-3127 [PMID:7932535] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opoid receptor in Dunkin-Hartley guinea pig brain after 1 hr by liquid scintillation spectrometry | B | 6.33 | pKi | 468 | nM | Ki | J Med Chem (2013) 56: 4840-4848 [PMID:23517479] |
| ChEMBL | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor kappa 1 using [3H]- U-69,593 as radioligand | B | 6.33 | pKi | 467.74 | nM | Ki | J Med Chem (2002) 45: 1949-1956 [PMID:11960505] |
| ChEMBL | Activity was evaluated by inhibition of the binding of 1 nM [3H]U-69593 at Opioid receptor kappa 1 binding site | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (1996) 39: 1956-1966 [PMID:8642554] |
| ChEMBL | Receptor binding affinity towards opioid receptor kappa | B | 6.52 | pKi | 301 | 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 | 6.52 | pKi | 301 | nM | Ki | J Med Chem (1991) 34: 2624-2633 [PMID:1652025] |
| ChEMBL | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | B | 6.73 | pKi | 188 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand | B | 6.78 | pKi | 167 | nM | Ki | J Med Chem (1988) 31: 555-560 [PMID:2831363] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptors in guine pig brain (minus cerebellum). | B | 6.82 | pKi | 151 | nM | Ki | J Med Chem (1991) 34: 397-403 [PMID:1846921] |
| ChEMBL | Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig | B | 6.82 | pKi | 151 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Inhibition of [3H]U-69593 binding to opioid receptor kappa from guinea pig brain membranes | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (2005) 48: 3372-3378 [PMID:15857143] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 in guinea pig brain membranes | B | 6.96 | pKi | 110 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| ChEMBL | Binding affinity for the Opioid receptor kappa 1 | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Binding affinity towards Opioid receptor kappa 1 using [3H]U-69593 as radioligand. | B | 7.16 | pKi | 69.1 | nM | Ki | J Med Chem (1995) 38: 1547-1557 [PMID:7739013] |
| ChEMBL | Displacement of [3H]-U69593 from kappa opioid receptor in guinea pig cerebellum homogenates | B | 7.27 | pKi | 54.3 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4023-4026 [PMID:21641219] |
| ChEMBL | Binding affinity towards opioid receptor kappa 1 | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting | B | 7.33 | pKi | 46.9 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4104-4107 [PMID:21641798] |
| ChEMBL | Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| ChEMBL | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 7.46 | pKi | 35 | nM | Ki | Medchemcomm (2016) 7: 2368-2380 |
| ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting analysis | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2019) 62: 4204-4217 [PMID:30939014] |
| ChEMBL | Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain | B | 7.47 | pKi | 33.9 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes | B | 7.55 | pKi | 28.1 | nM | Ki | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| ChEMBL | Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593 | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1717-1721 [PMID:11425545] |
| ChEMBL | Binding affinity to displace radioligand [3H]U-69593 on Opioid receptor kappa 1 in guinea pig membranes. | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2000) 43: 3558-3565 [PMID:11000010] |
| ChEMBL | Displacement of [3H]U69593 form kappa opioid receptor in guinea pig brain | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Compound was evaluated for the opioid receptor kappa affinity using guinea pig brain membranes. | B | 5.62 | pIC50 | 2390 | 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 | 5.62 | pIC50 | 2390 | nM | IC50 | J Med Chem (1991) 34: 3149-3158 [PMID:1659636] |
| ChEMBL | Evaluated for the inhibition of [3H]EKC binding to Opioid receptor kappa 1 of guinea pig brain | B | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (1987) 30: 1538-1542 [PMID:2887656] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 6.3 | pIC50 | <500 | nM | IC50 | Bioorg Med Chem (2008) 16: 4304-4312 [PMID:18337104] |
| ChEMBL | Inhibition of [3H]- U69,593 binding to Guinea pig Opioid receptor kappa 1 | B | 6.57 | pIC50 | 271 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig cerebellum | B | 6.67 | pIC50 | 213.1 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6398-6401 [PMID:18990576] |
| ChEMBL | Binding to kappa opioid receptor by using [3H]U-69593 as radioligand in guinea pig cerebellum | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2527-2532 |
| ChEMBL | Inhibition of [3H]U-69593 radioligand binding to Guinea pig opioid receptor kappa 1. | B | 8.74 | pIC50 | 1.82 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| 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 | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
| ChEMBL | Displacement of [3H]naloxone from MOR (unknown origin) expressed in human 293T cells | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2015) 58: 2584-2608 [PMID:25494650] |
| ChEMBL | Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor mu 1 expressed in CHO cell membrane;Range is in between (6.8-43) | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| ChEMBL | In vitro potency was measured against human Opioid receptor mu 1 | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Displacement of [3H]-DAMGO from full length human MOR expressed in chem5 cells incubated for 60 mins by liquid scintillation counter | B | 8.22 | pKi | 6.08 | nM | Ki | Eur J Med Chem (2019) 182: 111634-111634 [PMID:31472474] |
| ChEMBL | Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO-K1 cells by scintillation counting analysis | B | 8.28 | pKi | 5.2 | nM | Ki | J Med Chem (2014) 57: 6845-6860 [PMID:25062506] |
| ChEMBL | Displacement of [3H]naloxone from human mu opioid receptor expressed in CHO-K1 cells after 150 mins by liquid scintillation counting method | B | 8.28 | pKi | 5.2 | nM | Ki | Medchemcomm (2016) 7: 317-326 |
| ChEMBL | Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells | B | 8.34 | pKi | 4.6 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of [3H]diprenorphine from human MOR expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting assay | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2020) 63: 1671-1683 [PMID:31986033] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | B | 8.38 | pKi | 4.19 | nM | Ki | J Nat Prod (2021) 84: 1034-1043 [PMID:33635670] |
| ChEMBL | Displacement of [3H]naloxone from human mu poioid receptor expressed in HEK293 cells | B | 8.4 | pKi | 4 | nM | Ki | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
| ChEMBL | Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes incubated for 1 hr by scintillation counting method | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2018) 151: 495-507 [PMID:29649744] |
| ChEMBL | Binding affinity for Opioid receptor mu 1 | B | 8.4 | pKi | 3.96 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3141-3143 [PMID:12372519] |
| ChEMBL | Binding affinity determined against Opioid receptor mu 1 from human cloned receptor | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Binding affinity to MOP (unknown origin) | B | 8.55 | pKi | 2.84 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 8.59 | pKi | 2.6 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 8.59 | pKi | 2.6 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
| 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 | 8.59 | pKi | 2.6 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem (2011) 19: 3434-3443 [PMID:21570305] |
| 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 | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
| ChEMBL | Displacement of [125I]IOXY from human mu opioid receptor expressed in CHO cells coexpressing human recombinant MOR after 2 hrs by liquid scintillation counting | B | 8.59 | pKi | 2.55 | nM | Ki | Bioorg Med Chem (2011) 19: 4330-4337 [PMID:21684752] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells | B | 8.59 | pKi | 2.55 | nM | Ki | J Med Chem (2009) 52: 7570-7579 [PMID:19627147] |
| ChEMBL | Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells | B | 8.6 | pKi | 2.52 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK-293 cells by scintillation counting | B | 8.66 | pKi | 2.2 | nM | Ki | ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459] |
| ChEMBL | Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells | B | 8.72 | pKi | 1.92 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Binding affinity towards mu opioid receptor was determined | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1989) 32: 1620-1626 [PMID:2567782] |
| ChEMBL | Displacement of [3H]diprenorphine from recombinant mu opioid receptor expressed in C6 cells | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2008) 51: 2316-2320 [PMID:18311899] |
| ChEMBL | Displacement of [3H]DAMGO from human cloned mu opioid receptor | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cells | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
| GtoPdb | - | - | 9 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Mol Pharmacol (1989) 36: 265-72 [PMID:2549383] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (2012) 55: 3878-3890 [PMID:22439881] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (2006) 49: 256-262 [PMID:16392810] |
| ChEMBL | Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of Chinese hamster ovary membrane | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (2004) 47: 1886-1888 [PMID:15055988] |
| ChEMBL | Binding affinity to human mu opioid receptor | B | 9.28 | pKi | 0.53 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
| ChEMBL | null: The Ki (binding affinity) for u opioid receptors was determined using a competitive displacement assay as previously described in Neumeyer (Journal of Med. Chem. 2012, p 3878), which is incorporated herein in its entirety. Briefly, membrane protein from CHO (Chinese Hamster Ovarian) cells that stably expressed the cloned human u opioid receptor were incubated with 12 different concentrations of the compound set forth herein in the presence of 0.25 nM [3H]DAMGO (see Tiberi et al., Can. J. Physiol. Pharmacol. 1988, Vol. 66, p 1368, which is incorporated by reference herein in its entirety) in a final volume of 1 mL of 50 mM Tris-HCl, pH 7.5 at 25° C. Incubation times of 60 min were used for [3H]DAMGO (see Gulati et al., Life Sci. 1990, Vol. 47, p 159, which is incorporated by reference herein in its entirety). Nonspecific binding was measured by inclusion of 10 uM naloxone. The binding was terminated by filtering the samples through Schleicher & Schuell No. 32 glass fiber. | B | 9.49 | pKi | 0.32 | nM | Ki | US-9133125-B2. Morphan and morphinan analogues, and methods of use (2015) |
| ChEMBL | Displacement of [3H]DAMGO from mu-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | B | 9.85 | pKi | 0.14 | nM | Ki | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as induction of membrane potential change measured every 3 secs for 30 secs by fluorescent membrane potential assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | J Med Chem (2016) 59: 1239-1245 [PMID:26789491] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins by cAMP EIA | F | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (2012) 55: 10292-10296 [PMID:22995061] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method | F | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
| ChEMBL | Displacement of radiolabeled DAMGO from human recombinant mu opioid receptor expressed in OPRM1 cells | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | In vitro binding affinity against cloned human Opioid receptor mu 1 expressed in HEK 293S cells | B | 9.24 | pIC50 | 0.57 | nM | IC50 | J Med Chem (2003) 46: 34-48 [PMID:12502358] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay | B | 6.3 | pEC50 | 501.19 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Nb33 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | F | 6.38 | pEC50 | 416.87 | nM | EC50 | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in human USOS-beta-arrestin-hMOR-PathHunter cells incubated for 90 mins by beta-arrestin-2 enzyme fragment complementation assay | F | 6.42 | pEC50 | 379 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 6.5 | pEC50 | 316 | nM | EC50 | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins | F | 6.5 | pEC50 | 316 | nM | EC50 | J Med Chem (2011) 54: 980-988 [PMID:21235243] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay | F | 6.83 | pEC50 | 147 | nM | EC50 | J Med Chem (2020) 63: 1671-1683 [PMID:31986033] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as arrestin-3 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | F | 7.1 | pEC50 | 79.43 | nM | EC50 | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| ChEMBL | Agonist activity at MOR (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 | 7.15 | pEC50 | 71.6 | nM | EC50 | J Med Chem (2021) 64: 13394-13409 [PMID:34465090] |
| ChEMBL | Agonist activity at MOR (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 | 7.15 | pEC50 | 70.79 | nM | EC50 | J Med Chem (2021) 64: 13394-13409 [PMID:34465090] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by scintillation counting method | F | 7.19 | pEC50 | 64 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| ChEMBL | Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes. | F | 7.47 | pEC50 | 34 | nM | EC50 | US-9133125-B2. Morphan and morphinan analogues, and methods of use (2015) |
| ChEMBL | Agonist activity at mu-opioid receptor (unknown origin) | F | 7.68 | pEC50 | 21 | nM | EC50 | J Med Chem (2023) 66: 16257-16275 [PMID:38015878] |
| ChEMBL | Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay | F | 7.68 | pEC50 | 21 | nM | EC50 | J Med Chem (2023) 66: 16257-16275 [PMID:38015878] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.81 | pEC50 | 15.6 | nM | EC50 | J Med Chem (2009) 52: 1553-1557 [PMID:19253983] |
| ChEMBL | Stimulation of [35S]GTPgammaS binding to human recombinant MOR | F | 7.81 | pEC50 | 15.6 | nM | EC50 | J Med Chem (2006) 49: 5333-5338 [PMID:16913723] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.81 | pEC50 | 15.6 | nM | EC50 | J Med Chem (2007) 50: 5176-5182 [PMID:17887741] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem (2014) 22: 4694-4703 [PMID:25087049] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | F | 8.06 | pEC50 | 8.71 | nM | EC50 | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| ChEMBL | Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay | F | 8.15 | pEC50 | 7 | nM | EC50 | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
| ChEMBL | Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM | B | 8.19 | pEC50 | 6.4 | nM | EC50 | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
| ChEMBL | Activation of human mu opioid receptor expressed in HEK293a cells co-expressing YFP-labelled alphai1 and CFP-labelled beta1gamma2 Gi subunits assessed as Gi protein activation by fluorescence resonance energy transfer | B | 8.22 | pEC50 | 6 | nM | EC50 | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
| ChEMBL | Agonist activity at human mu 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 | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| ChEMBL | Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | F | 8.33 | pEC50 | 4.7 | nM | EC50 | RSC Med Chem (2020) 11: 896-904 [PMID:33479684] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay | F | 8.43 | pEC50 | 3.7 | nM | EC50 | ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459] |
| Mu opioid receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3041] [UniProtKB: P79350] | ||||||||
| ChEMBL | Binding affinity towards opioid receptor mu 2 | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| ChEMBL | Activity was evaluated by inhibition of the binding of 0.8 nM [3H]- DAMGO at Opioid receptor mu 1 binding site | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1996) 39: 1956-1966 [PMID:8642554] |
| ChEMBL | Binding affinity towards opioid receptor mu 1 | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [125I]BNtxA from mouse MOR expressed in CHO cell membranes after 90 mins by filter binding assay | B | 8.34 | pKi | 4.6 | nM | Ki | Medchemcomm (2017) 8: 152-157 [PMID:28603600] |
| ChEMBL | Binding affinity against mu opioid receptor in mouse hot plate test | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5493-5498 [PMID:15482911] |
| ChEMBL | Compound was tested for irreversible antagonist activity at Opioid receptor mu 1 by determining by MVD response | F | 5.85 | pIC50 | 1420 | nM | IC50 | J Med Chem (1984) 27: 1325-1335 [PMID:6090663] |
| ChEMBL | Antagonist activity at mouse vas deferns MOP | F | 5.92 | pIC50 | 1215 | nM | IC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum | B | 8.9 | pIC50 | 1.27 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6398-6401 [PMID:18990576] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in ICR mouse whole brain | B | 8.9 | pIC50 | 1.27 | nM | IC50 | Bioorg Med Chem (2008) 16: 4304-4312 [PMID:18337104] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 6.31 | pEC50 | 491 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 6.31 | pEC50 | 489.78 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Agonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as inhibition of electrically-stimulated twitch | F | 6.4 | pEC50 | 395 | nM | EC50 | Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 6.68 | pEC50 | 208.93 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 6.68 | pEC50 | 207 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay | F | 6.92 | pEC50 | 120 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| ChEMBL | Agonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 7.07 | pEC50 | 85.5 | nM | EC50 | Bioorg Med Chem (2010) 18: 3535-3542 [PMID:20413312] |
| ChEMBL | Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| ChEMBL | Partial agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 7.92 | pEC50 | 12.1 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 7.92 | pEC50 | 12.02 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| ChEMBL | Displacement of [3H]diprenorphine from rat mu receptor expressed in CHO cells by scintillation counting | B | 6.93 | pKi | 116.8 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 418-421 [PMID:19932964] |
| ChEMBL | Displacement of [3H]diprenorphine from N-terminal HA epitope-tagged rat mu opioid receptor expressed in HEK293 cells by scintillation counting | B | 6.95 | pKi | 113 | nM | KiL | J Med Chem (2009) 52: 2656-2666 [PMID:19351163] |
| ChEMBL | Binding affinity for mu opioid receptor was evaluated by displacing [3H]- diprenorphine | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1993) 36: 1860-1865 [PMID:8390575] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| ChEMBL | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 using [3H]DAMGO as radioligand. | B | 8.09 | pKi | 8.14 | nM | Ki | J Med Chem (1995) 38: 1547-1557 [PMID:7739013] |
| ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method | B | 8.16 | pKi | 6.9 | nM | Ki | J Med Chem (2021) 64: 12414-12433 [PMID:34387468] |
| ChEMBL | In vitro binding affinity at opioid receptor mu 1 was determined in C6 rat glioma cells using [3H]DAMGO | B | 8.18 | pKi | 6.55 | nM | Ki | J Med Chem (2003) 46: 1758-1763 [PMID:12699394] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 isolated from rat brain membrane was determined using [3H]DAMGO as radioligand | B | 8.18 | pKi | 6.55 | nM | Ki | J Med Chem (2003) 46: 4182-4187 [PMID:12954070] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor of rat brain membranes | B | 8.18 | pKi | 6.55 | nM | Ki | J Med Chem (2005) 48: 5052-5055 [PMID:16033285] |
| ChEMBL | Inhibition of [3H]DAMGO binding to opioid receptor mu from rat brain membranes | B | 8.18 | pKi | 6.55 | nM | Ki | J Med Chem (2005) 48: 3372-3378 [PMID:15857143] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain membrane by liquid scintillation counting | B | 8.18 | pKi | 6.55 | nM | Ki | J Med Chem (2011) 54: 980-988 [PMID:21235243] |
| ChEMBL | Displacement of [3H]diprenorphine from rat MOR expressed in rat C6 cells after 1 hr by liquid scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2013) 56: 2139-2149 [PMID:23419026] |
| ChEMBL | Displacement of [3H]-diprenorphine from rat mu-type opioid receptor expressed in rat C6 cell membranes incubated for 1 hr by liquid scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2019) 62: 4142-4157 [PMID:30924650] |
| ChEMBL | Binding affinity to Opioid receptor mu 1 in rat brain using [3H]-NAL as radioligand | B | 8.24 | pKi | 5.7 | nM | Ki | J Med Chem (1988) 31: 555-560 [PMID:2831363] |
| ChEMBL | mu-2 receptor binding affinity in rat brain by 3H [d-Ala2, (N-Me)Phe4, Gly5-ol] enkephalin displacement. | B | 8.32 | pKi | 4.8 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1207-1214 [PMID:12643945] |
| ChEMBL | Inhibition of [3H]dihydromorphine (1 nM) binding to mu opioid receptor of rat brain homogenate | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 589-592 |
| ChEMBL | Inhibition of [3H]DAMGO binding to rat brain homogenat Opioid receptor mu 1 | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (2000) 43: 2115-2123 [PMID:10841790] |
| ChEMBL | Displacement of [3H]diprenorphine from N-terminal HA epitope-tagged rat mu opioid receptor expressed in HEK293 cells by scintillation counting | B | 8.6 | pKi | 2.5 | nM | KiH | J Med Chem (2009) 52: 2656-2666 [PMID:19351163] |
| ChEMBL | Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes | B | 8.67 | pKi | 2.15 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes. | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1990) 33: 2876-2882 [PMID:2170652] |
| ChEMBL | Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1994) 37: 2678-2685 [PMID:8064796] |
| ChEMBL | Inhibition of binding of [3H]DAMGO to opioid receptor mu 1 from rat brain membrane. | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1741-1743 [PMID:11425550] |
| ChEMBL | Binding affinity by inhibition of [3H]DAMGO binding to Opioid receptor mu 1 from rat brain membranes | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1109-1111 [PMID:10843229] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes | B | 8.84 | pKi | 1.45 | nM | Ki | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| ChEMBL | Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2003) 46: 623-633 [PMID:12570383] |
| ChEMBL | mu-1 receptor binding affinity in rat brain by 3H [d-Ala2, d-Leu5] enkephalin displacement. | B | 9.11 | pKi | 0.78 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1207-1214 [PMID:12643945] |
| ChEMBL | Displacement of [3H]naloxone from mu opioid receptor in rat brain membrane | B | 5.01 | pIC50 | 9770 | nM | IC50 | J Med Chem (2008) 51: 2571-2574 [PMID:18370374] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor from Wistar rat brain by liquid scintillation counting | B | 8.25 | pIC50 | 5.64 | nM | IC50 | Bioorg Med Chem (2010) 18: 3535-3542 [PMID:20413312] |
| ChEMBL | Displacement of [3H]- DAGO from opioid receptor mu in rat brain membrane | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
| ChEMBL | Inhibition of [3H]DAMGO radioligand binding to rat brain opioid receptor mu 1. | B | 8.71 | pIC50 | 1.94 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| ChEMBL | Inhibition of [3H]- DAMGO binding to Rat brain Opioid receptor mu 1 | B | 8.71 | pIC50 | 1.94 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | Opioid receptor activity in terms of inhibition of [3H]dihydromorphine binding in rat brain membrane | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (1991) 34: 194-197 [PMID:1671414] |
| ChEMBL | Inhibition of [3H]DAMGO radioligand binding to rat brain opioid receptor mu 1. | B | 9.85 | pIC50 | 0.14 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| ChEMBL | Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis | F | 6.71 | pEC50 | 194 | nM | EC50 | J Med Chem (2013) 56: 2139-2149 [PMID:23419026] |
| ChEMBL | Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method | F | 6.71 | pEC50 | 194 | nM | EC50 | J Med Chem (2019) 62: 4142-4157 [PMID:30924650] |
| ChEMBL | Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding | F | 6.91 | pEC50 | 123.5 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 418-421 [PMID:19932964] |
| ChEMBL | Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting | F | 6.91 | pEC50 | 123.5 | nM | EC50 | J Med Chem (2019) 62: 11054-11070 [PMID:31738550] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | F | 6.91 | pEC50 | 123.5 | nM | EC50 | J Med Chem (2021) 64: 12414-12433 [PMID:34387468] |
| ChEMBL | Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor | F | 7.67 | pEC50 | 21.3 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against mu opioid receptor was determined in brain membrane preparations from male Hartley guinea-pigs | B | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439] |
| ChEMBL | In vivo binding affinity against mu opioid receptor was measured by using labeled ligand [3H]naloxone (0.5 nM) | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (1994) 37: 3121-3127 [PMID:7932535] |
| ChEMBL | Binding affinities against Opioid receptor mu 1 of guinea pig brain membrane using [3H]DAGO as the radioligand using competition binding assays. | B | 8.11 | pKi | 7.71 | nM | Ki | J Med Chem (1990) 33: 206-212 [PMID:1967312] |
| ChEMBL | Binding affinity against mu opioid receptor in guinea pig brain membranes | B | 8.19 | pKi | 6.51 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| ChEMBL | Displacement of [3H]DAMGO from mu-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting | B | 8.28 | pKi | 5.2 | nM | Ki | J Med Chem (2017) 60: 2526-2551 [PMID:28218838] |
| ChEMBL | Displacement of [3H]-DAMGO from MOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay | B | 8.28 | pKi | 5.2 | nM | Ki | Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 8.41 | pKi | 3.9 | nM | Ki | Medchemcomm (2016) 7: 2368-2380 |
| ChEMBL | Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2019) 62: 4204-4217 [PMID:30939014] |
| ChEMBL | Displacement of [3H]DAMGO from mu opoid receptor in Dunkin-Hartley guinea pig brain after 1.5 hrs by liquid scintillation spectrometry | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2013) 56: 4840-4848 [PMID:23517479] |
| ChEMBL | Inhibition of mu opioid receptor in guinea pig brain membranes | B | 8.46 | pKi | 3.5 | nM | Ki | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| ChEMBL | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor mu 1 using [3H]- DAMGO as radioligand | B | 8.46 | pKi | 3.47 | nM | Ki | J Med Chem (2002) 45: 1949-1956 [PMID:11960505] |
| ChEMBL | Receptor binding affinity towards opioid receptor mu | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (1992) 35: 2970-2978 [PMID:1323679] |
| ChEMBL | Displacement of [3H]DAGO from mu opioid receptors in guinea pig brain (minus cerebellum). | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (1991) 34: 397-403 [PMID:1846921] |
| ChEMBL | Affinity for opioid receptor mu sites | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (1991) 34: 2624-2633 [PMID:1652025] |
| ChEMBL | Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig | B | 8.52 | pKi | 3 | 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 | 8.6 | pKi | 2.5 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2011) 46: 1972-1982 [PMID:21481987] |
| ChEMBL | Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig forebrain homogenates | B | 8.7 | pKi | 1.98 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4023-4026 [PMID:21641219] |
| ChEMBL | Binding affinity for the Opioid receptor mu 1 | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4104-4107 [PMID:21641798] |
| ChEMBL | Displacement of [3H]DAMGO form mu opioid receptor in guinea pig brain | B | 9.06 | pKi | 0.88 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 of guinea pig brain membranes using radioligand 0.25 nM [3H]DAMGO | B | 9.06 | pKi | 0.88 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1717-1721 [PMID:11425545] |
| ChEMBL | Binding affinity to displace radioligand [3H]DAMGO on Opioid receptor mu 1 in guinea pig membranes. | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (2000) 43: 3558-3565 [PMID:11000010] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum | F | 4.53 | pIC50 | 29300 | nM | IC50 | J Med Chem (2008) 51: 2571-2574 [PMID:18370374] |
| ChEMBL | In vitro agonistic activity against opioid receptor mu of guinea pig ileum | F | 6.51 | pIC50 | 311 | nM | IC50 | J Med Chem (2005) 48: 3372-3378 [PMID:15857143] |
| ChEMBL | Antagonist activity at guinea pig ileum MOP | F | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Ability to induce 50% of maximal effect in guinea pig ileum expressing Opioid receptor mu 1 | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (1983) 26: 1643-1645 [PMID:6313921] |
| ChEMBL | Evaluated for inhibitory activity against Opioid receptor mu 1 of guinea pig ileum (GPI) | B | 7.15 | pIC50 | 71.6 | nM | IC50 | J Med Chem (1990) 33: 206-212 [PMID:1967312] |
| ChEMBL | Inhibitory potency against Opioid receptor mu 1 in longitudinal muscle preparation of guinea pig ileum | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (1981) 24: 1119-1124 [PMID:6276540] |
| ChEMBL | Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors | F | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Ability to inhibit electrically evoked contractions of isolated muscle preparations of guinea pig ileum (GPI, mu receptor) | F | 7.23 | pIC50 | 58.8 | nM | IC50 | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| ChEMBL | Mu opioid receptor agonist activity as inhibition of electrically stimulated mysenteric plexus in guinea pig ileum | F | 7.24 | pIC50 | 57.3 | nM | IC50 | J Med Chem (1982) 25: 1423-1427 [PMID:7154002] |
| ChEMBL | Inhibition of opioid receptor mu in guinea pig ileum (GPI) | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | B | 7.53 | pIC50 | 29.3 | nM | IC50 | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| ChEMBL | Binding to mu opioid receptor by using [3H]DAMGO as radioligand in guinea pig brain minus cerebellum | B | 8.07 | pIC50 | 8.5 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2527-2532 |
| ChEMBL | Evaluated for the inhibition of [3H]DAGO binding to mu-receptor of guinea pig brain | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1987) 30: 1538-1542 [PMID:2887656] |
| α2A-adrenoceptor/μ receptor/Mu opioid receptor/Alpha-2A adrenergic receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883321] [GtoPdb: 25, 319] [UniProtKB: P08913, P35372] | ||||||||
| GtoPdb | - | - | 9 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Mol Pharmacol (1989) 36: 265-72 [PMID:2549383] |
| ChEMBL | Inhibition of MOR/alpha2A adrenergic receptor heterodimer expressed in HEK293 cells assessed as stimulation of ERK1/2 phosphorylation | B | 8.52 | pEC50 | 3 | nM | EC50 | Nat Chem Biol (2008) 4: 126-131 [PMID:18193048] |
| α2A-adrenoceptor/μ receptor in Rat [GtoPdb: 25, 319] [UniProtKB: P22909, P33535] | ||||||||
| GtoPdb | - | - | 7.9 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| Mu opioid receptor-like OR2 in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3611961] [UniProtKB: Q98UH1] | ||||||||
| ChEMBL | Displacement of [3H]-diprenorphine from zebrafish mu opioid receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting | B | 6.73 | pKi | 187.4 | nM | Ki | Eur J Med Chem (2015) 101: 150-162 [PMID:26134550] |
| ChEMBL | Displacement of [3H]DPN from zebrafish mu opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method | B | 6.73 | pKi | 187 | nM | Ki | Bioorg Med Chem (2017) 25: 2260-2265 [PMID:28284867] |
| 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 | 7.86 | pKi | 13.9 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| Opioid receptor, delta 1b in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105711] [UniProtKB: B3DH72] | ||||||||
| ChEMBL | Displacement of [3H]DPN from zebrafish delta 1b opioid receptor expressed in HEK293 cell membranes after 4 hrs by scintillation counting method | B | 5.85 | pKi | 1427 | nM | Ki | Bioorg Med Chem (2017) 25: 2260-2265 [PMID:28284867] |
| Opioid receptor homologue in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105897] [UniProtKB: O57585] | ||||||||
| ChEMBL | Displacement of [3H]DPN from zebrafish delta 1a opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method | B | 6.65 | pKi | 223 | nM | Ki | Bioorg Med Chem (2017) 25: 2260-2265 [PMID:28284867] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | In vivo binding affinity against sigma Opioid receptor was measured by using labeled ligand [3H]-SKF- 10,047 (1 nM) | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1994) 37: 3121-3127 [PMID:7932535] |
| ChEMBL | Compound was evaluated for the binding affinity to sigma opioid receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 715-720 |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | B | 4.14 | pIC50 | 71790 | nM | IC50 | J Med Chem (2019) 62: 9890-9905 [PMID:31597043] |
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.55 | pIC50 | 28000 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
