DAMGO [Ligand Id: 1647] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38874 (DAMGO) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Binding affinity to adenosine receptor A1 | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950] |
| CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from CCK2R-MOPR coexpressed in CHO cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2009) 52: 247-258 [PMID:19113864] |
| ChEMBL | Activity at CCK2R-MOPR coexpressed in CHO cells co-transfected with delta-6-Galphaqi4-myr assessed as intracellular calcium release by FLIPR | F | 8.58 | pEC50 | 2.66 | nM | EC50 | J Med Chem (2009) 52: 247-258 [PMID:19113864] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | F | 5.73 | pKd | 1850 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | F | 5.73 | pKd | 1850 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | In vitro potency was measured against human Opioid receptor delta 1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 | B | 5.7 | pKi | >2000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
| ChEMBL | Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 5.82 | pKi | 1500 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
| 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 | 5.82 | pKi | 1500 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
| ChEMBL | Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5.82 | pKi | 1500 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
| 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 | 5.82 | pKi | 1500 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
| ChEMBL | Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting analysis | B | 6 | pKi | 990 | nM | Ki | J Med Chem (2015) 58: 5728-5741 [PMID:26125201] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 | B | 6.25 | pKi | 567 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2681-2684 [PMID:9873602] |
| ChEMBL | Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Binding affinity for delta opioid receptor | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1585-1589 [PMID:12699761] |
| ChEMBL | Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain | B | 6.9 | pKi | 127 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | B | 9.18 | pKi | 0.66 | nM | Ki | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | B | 8.84 | pIC50 | 1.45 | nM | IC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| ChEMBL | Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 8.16 | pEC50 | 6.86 | nM | EC50 | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [125I]-Deltorphin 2 from mouse Flag-tagged delta-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting | B | 5.81 | pIC50 | 1533 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
| ChEMBL | Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions | F | 6.02 | pIC50 | 950 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
| ChEMBL | Displacement of [3H]DPDPE from Sprague-Dawley rat delta opioid receptor by liquid scintillation counting | B | 5.57 | pKi | 2670 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 by displacement of radioligand [3H]DSLET in rat brain membrane | B | 5.89 | pKi | 1280 | nM | Ki | J Med Chem (1989) 32: 698-703 [PMID:2537427] |
| ChEMBL | Ability to inhibit the binding of [3H]DSLET to Opioid receptor delta 1 in rat brain membranes | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Binding affinity to opioid receptor delta was determined in rat brain using [3H]DSTBULET as radioligand | B | 6.2 | pKi | 629 | nM | Ki | J Med Chem (1991) 34: 2430-2438 [PMID:1714957] |
| ChEMBL | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | B | 6.33 | pKi | 469 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 in P2 membrane preparation of rat brain by [3H]DADLE displacement. | B | 6.74 | pKi | 180.4 | nM | Ki | J Med Chem (1991) 34: 1350-1355 [PMID:1849997] |
| ChEMBL | Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane | B | 6.14 | pIC50 | 727 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
| ChEMBL | Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay | F | 7.31 | pEC50 | 49 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | In vitro potency was measured against human Opioid receptor kappa 1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 | B | 5.7 | pKi | >2000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
| ChEMBL | Binding affinity for kappa opioid receptor | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1585-1589 [PMID:12699761] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 6.51 | pKi | 306 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | B | 6.52 | pKi | 305 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting analysis | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2015) 58: 5728-5741 [PMID:26125201] |
| 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 | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| ChEMBL | Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. | B | 5.36 | pEC50 | 4365 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | F | 6.29 | pKd | 509 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | F | 6.29 | pKd | 509 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | B | 5.24 | pKi | 5820 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Displacement of [3H]U69593 from Sprague-Dawley rat kappa opioid receptor in guinea pig cerebella by liquid scintillation counting | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain | B | 5.73 | pKi | 1841 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysis | B | 5.66 | pKi | 2187.76 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| ChEMBL | Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexyl)-amino)-6-oxohexyl)-3,3-dimethyl-3H-indol-1-ium-5-sulfonate,2,2,2-Trifluoroacetate Salt from human MOR expressed in HEK293 cells by Cheng-Prusoff analysis | B | 7.06 | pKi | 87.1 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| ChEMBL | Inhibition of [3H]diprenorphine binding to human Opioid receptor mu 1 | B | 7.44 | pKi | 36.7 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
| ChEMBL | In vitro potency was measured against human Opioid receptor mu 1 | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins | B | 8.09 | pKi | 8.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells | B | 8.17 | pKi | 6.7 | nM | Ki | J Med Chem (2009) 52: 247-258 [PMID:19113864] |
| ChEMBL | Binding affinity to mu opioid receptor | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950] |
| ChEMBL | Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in in CHO cells | B | 8.43 | pKi | 3.71 | nM | Ki | Bioorg Med Chem (2007) 15: 4434-4443 [PMID:17490886] |
| ChEMBL | Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells | B | 8.48 | pKi | 3.34 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor transfected in CHO cell membranes after 60 mins | B | 8.53 | pKi | 2.96 | nM | Ki | Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2014) 85: 818-829 [PMID:25193297] |
| ChEMBL | Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 8.8 | pKi | 1.59 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells | B | 8.81 | pKi | 1.55 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in CHO cells | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 666-669 [PMID:28011222] |
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 2 hrs by liquid scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2012) 55: 10292-10296 [PMID:22995061] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cells by scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2014) 57: 6861-6866 [PMID:25051243] |
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| 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 | 8.92 | pKi | 1.2 | 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 cell membranes after 2 hrs by liquid scintillation counting analysis | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
| ChEMBL | Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay | B | 9.19 | pKi | 0.64 | nM | Ki | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Displacement of [3H]DAMGO from MOR in HEK293 cells | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem (2016) 24: 5280-5290 [PMID:27624520] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting analysis | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (2015) 58: 5728-5741 [PMID:26125201] |
| ChEMBL | Binding affinity for mu opioid receptor | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1585-1589 [PMID:12699761] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Eur J Pharmacol (1981) 70: 531-40 [PMID:6263640] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells | B | 9.35 | pKi | 0.45 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of radiolabeled DAMGO from human mu-type opioid receptor agonist site | F | 9.36 | pKi | 0.44 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | B | 9.39 | pKi | 0.4 | nM | Ki | J Nat Prod (2021) 84: 1034-1043 [PMID:33635670] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO-K1 cells by radioligand binding assay | B | 9.46 | pKi | 0.35 | nM | Ki | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO-K1 cells by radioligand binding assay | B | 9.5 | pKi | 0.32 | nM | Ki | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Binding affinity to human mu-type opioid receptor by radioligand displacement assay | B | 9.55 | pKi | 0.28 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method | F | 7.71 | pIC50 | 19.3 | nM | IC50 | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay | F | 8.29 | pIC50 | 5.1 | nM | IC50 | Eur J Med Chem (2017) 126: 202-217 [PMID:27776274] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2014) 22: 4694-4703 [PMID:25087049] |
| ChEMBL | Agonist activity at mu opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 8.5 | pIC50 | 3.18 | nM | IC50 | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| 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 | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2016) 59: 1239-1245 [PMID:26789491] |
| ChEMBL | Inhibition of human mu opioid receptor | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Displacement of [3H]naloxone from mu opioid receptor expressed in CHO cell membrane | B | 8.7 | pIC50 | 2 | nM | IC50 | J Nat Prod (2010) 73: 988-991 [PMID:20426456] |
| ChEMBL | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay | F | 8.71 | pIC50 | 1.95 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209] |
| ChEMBL | Binding activity against human Opioid receptor mu 1 using [3H]DAMGO as a radioligand | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2002) 45: 1395-1398 [PMID:11906279] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation after 15 mins by EIA | F | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
| ChEMBL | Displacement of radiolabeled DAMGO from human mu-type opioid receptor agonist site | F | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay | F | 9.1 | pIC50 | 0.79 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209] |
| ChEMBL | Binding affinity to mu opioid receptor (unknown origin) by radioligand displacement assay | B | 9.13 | pIC50 | 0.74 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Binding affinity to human mu-type opioid receptor by radioligand displacement assay | B | 9.17 | pIC50 | 0.68 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu-opioid receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant Mu-type opioid receptor expressed in CHO cells | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| 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 | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| ChEMBL | Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor mu 1 | B | 6.69 | pEC50 | 202 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay | F | 6.7 | pEC50 | 199.53 | nM | EC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay | F | 6.74 | pEC50 | 182.04 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| ChEMBL | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay | F | 6.74 | pEC50 | 181.97 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| ChEMBL | Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2006) 49: 256-262 [PMID:16392810] |
| ChEMBL | Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding | F | 6.96 | pEC50 | 110 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1508-1511 [PMID:17276685] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins | F | 6.96 | pEC50 | 110 | nM | EC50 | Bioorg Med Chem (2007) 15: 4106-4112 [PMID:17433695] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2011) 54: 1903-1913 [PMID:21351746] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay | F | 7.22 | pEC50 | 60.9 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7340-7344 [PMID:23142613] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2006) 49: 5635-5639 [PMID:16942039] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6516-6520 [PMID:17935988] |
| ChEMBL | Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| ChEMBL | Activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem (2008) 16: 5653-5664 [PMID:18417347] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 365-368 [PMID:19091564] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2012) 55: 3878-3890 [PMID:22439881] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 2128-2133 [PMID:23434225] |
| ChEMBL | Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation [35S]GTPgammaS binding relative to basal level | F | 7.35 | pEC50 | 45.1 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280] |
| ChEMBL | Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.35 | pEC50 | 45.06 | nM | EC50 | J Med Chem (2009) 52: 1416-1427 [PMID:19199782] |
| ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.45 | pEC50 | 35.3 | nM | EC50 | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| 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 | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| ChEMBL | Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis | F | 7.49 | pEC50 | 32.6 | nM | EC50 | Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay | B | 7.52 | pEC50 | 30 | nM | EC50 | ACS Med Chem Lett (2016) 7: 391-396 [PMID:27096047] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 7.59 | pEC50 | 25.5 | nM | EC50 | J Med Chem (2020) 63: 7663-7694 [PMID:32530286] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | F | 7.64 | pEC50 | 23 | nM | EC50 | ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 7.71 | pEC50 | 19.7 | nM | EC50 | ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778] |
| ChEMBL | Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells | F | 7.86 | pEC50 | 13.7 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by cytosensor micrometer | F | 8.02 | pEC50 | 9.61 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| ChEMBL | Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.09 | pEC50 | 8.2 | nM | EC50 | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.12 | pEC50 | 7.57 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by microplate reader analysis | F | 8.12 | pEC50 | 7.5 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay | F | 8.14 | pEC50 | 7.2 | nM | EC50 | J Med Chem (2020) 63: 2673-2687 [PMID:31834798] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 8.2 | pEC50 | 6.38 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | F | 8.23 | pEC50 | 5.89 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting | F | 8.5 | pEC50 | 3.18 | nM | EC50 | J Med Chem (2011) 54: 7848-7859 [PMID:21978284] |
| ChEMBL | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter | F | 8.52 | pEC50 | 3.04 | nM | EC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
| ChEMBL | Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis | F | 8.52 | pEC50 | 3.04 | nM | EC50 | J Med Chem (2013) 56: 3102-3114 [PMID:23477419] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry | F | 8.71 | pEC50 | 1.97 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2008) 51: 4404-4411 [PMID:18637671] |
| 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 | 9 | pEC50 | 1 | nM | EC50 | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
| ChEMBL | Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay | F | 9 | pEC50 | 1 | 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 | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | F | 9.31 | pEC50 | 0.49 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| 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 | 9.52 | pEC50 | 0.3 | nM | EC50 | RSC Med Chem (2020) 11: 896-904 [PMID:33479684] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mouse whole brain MOR | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Agonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 7.12 | pIC50 | 75.55 | nM | IC50 | J Med Chem (2008) 51: 173-177 [PMID:18062664] |
| ChEMBL | Agonist activity at mouse HA-tagged mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay | F | 8.18 | pIC50 | 6.6 | nM | IC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Agonist activity at mouse HA-tagged mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay | F | 8.2 | pIC50 | 6.31 | nM | IC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
| ChEMBL | Displacement of [125I]-DAMGO from mouse Flag-tagged mu-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting | B | 8.86 | pIC50 | 1.39 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
| ChEMBL | Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy | F | 7.72 | pEC50 | 19 | nM | EC50 | Medchemcomm (2017) 8: 152-157 [PMID:28603600] |
| ChEMBL | Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP formation incubated for 8 min followed by forskolin stimulation by ELISA | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2019) 62: 11399-11415 [PMID:31782922] |
| ChEMBL | Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| ChEMBL | Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | F | 8.25 | pEC50 | 5.6 | nM | EC50 | Eur J Med Chem (2013) 69: 786-789 [PMID:24103580] |
| ChEMBL | Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
| ChEMBL | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | B | 8.21 | pKi | 6.1 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1994) 37: 2678-2685 [PMID:8064796] |
| ChEMBL | Binding affinity to opioid receptor mu was determined in rat brain using [3H]DAGO as radioligand | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1991) 34: 2430-2438 [PMID:1714957] |
| ChEMBL | Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Displacement of [3H]-DAMGO from rat mu opioid receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 8.77 | pKi | 1.7 | nM | Ki | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 | B | 8.79 | pKi | 1.64 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2755-2758 [PMID:11133084] |
| ChEMBL | Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2004) 47: 5198-5203 [PMID:15456262] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2002) 45: 2571-2578 [PMID:12036366] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 by displacement of radioligand [3H]-DAGO in rat brain membrane | B | 8.91 | pKi | 1.22 | nM | Ki | J Med Chem (1989) 32: 698-703 [PMID:2537427] |
| ChEMBL | Displacement of [3H]-DAMGO from MOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | B | 8.94 | pKi | 1.16 | nM | Ki | Eur J Med Chem (2019) 168: 189-198 [PMID:30822708] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | B | 9 | pKi | 1 | nM | Ki | ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662] |
| ChEMBL | Displacement of [3H]-DAMGO from MOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | B | 9.05 | pKi | 0.9 | nM | Ki | ACS Med Chem Lett (2020) 11: 678-685 [PMID:32435370] |
| ChEMBL | Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting | B | 9.06 | pKi | 0.87 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Displacement of [3H]DPDPE from rat mu opioid receptor | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement. | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (1991) 34: 1350-1355 [PMID:1849997] |
| ChEMBL | Compound was evaluated for the binding affinity of Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from rat brain membrane | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1185-1188 [PMID:10866377] |
| ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | B | 7.44 | pIC50 | 36.31 | nM | IC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
| ChEMBL | Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | B | 8 | pIC50 | 9.9 | nM | IC50 | J Med Chem (2002) 45: 2571-2578 [PMID:12036366] |
| ChEMBL | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 8 | pIC50 | 9.9 | nM | IC50 | J Med Chem (2004) 47: 5198-5203 [PMID:15456262] |
| ChEMBL | Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | B | 8 | pIC50 | 9.89 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2755-2758 [PMID:11133084] |
| ChEMBL | The compound was tested for binding affinity towards rat Opioid receptor mu 1 by displacing [3H]DAMGO. | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (1999) 42: 4331-4342 [PMID:10543877] |
| ChEMBL | Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2027-2032 [PMID:9873480] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 8.62 | pIC50 | 8.62 | - | logIC50 | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
| ChEMBL | Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane | B | 8.95 | pIC50 | 1.13 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain | B | 9 | pIC50 | 1.01 | nM | IC50 | Bioorg Med Chem (2009) 17: 5782-5790 [PMID:19640720] |
| ChEMBL | Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay | F | 6.31 | pEC50 | 485 | nM | EC50 | J Med Chem (2012) 55: 8418-8428 [PMID:22957923] |
| ChEMBL | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay | F | 6.67 | pEC50 | 214 | nM | EC50 | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
| ChEMBL | Agonist activity at rat mu 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 | 6.84 | pEC50 | 146 | nM | EC50 | Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512] |
| ChEMBL | Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding | F | 6.84 | pEC50 | 145 | nM | EC50 | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.09 | pEC50 | 81 | nM | EC50 | ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | F | 7.4 | pEC50 | 7.4 | nM | pEC50 | J Med Chem (2008) 51: 6334-6347 [PMID:18821747] |
| ChEMBL | Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay | F | 7.4 | pEC50 | -7.4 | - | logEC50 | J Med Chem (2008) 51: 1369-1376 [PMID:18266313] |
| ChEMBL | Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2006) 49: 2868-2875 [PMID:16686530] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2006) 49: 1773-1780 [PMID:16509592] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| ChEMBL | Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2008) 51: 1369-1376 [PMID:18266313] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2011) 54: 382-386 [PMID:21128594] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2008) 51: 6334-6347 [PMID:18821747] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2011) 54: 2029-2038 [PMID:21366266] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2006) 49: 1773-1780 [PMID:16509592] |
| ChEMBL | Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2006) 49: 2868-2875 [PMID:16686530] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2011) 54: 382-386 [PMID:21128594] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2011) 54: 2029-2038 [PMID:21366266] |
| ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | F | 8.09 | pEC50 | 8.06 | nM | EC50 | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
| ChEMBL | Agonist activity at rat mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay | F | 9.59 | pEC50 | 0.26 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.23 | pKd | 592 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.23 | pKd | 592 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Binding affinity against mu opioid receptor | B | 9 | pKi | 0.99 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2681-2684 [PMID:9873602] |
| ChEMBL | Agonist activity at mu-opioid receptor in guinea pig ileum assessed as inhibition of electrically induced contractions | F | 7.55 | pIC50 | 28.3 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
| ChEMBL | Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors | F | 7.94 | pIC50 | 11.5 | nM | IC50 | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Agonist activity at MOR in Dunkin-Hartley guinea pig ileum assessed as inhibition of EFS-induced contractions incubated for 60 mins | B | 6.8 | pEC50 | 158.49 | nM | EC50 | Bioorg Med Chem (2016) 24: 2832-2842 [PMID:27234885] |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Affinity for rat Tachykinin receptor 1 determined in displacement screening by using radioligand 3,4-[3H]-(L-Pro e2) SP. | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1999) 42: 4331-4342 [PMID:10543877] |
| NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
| ChEMBL | Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| Nociceptin receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5492] [UniProtKB: P47748] | ||||||||
| ChEMBL | Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain | B | 7.57 | pKi | 26.9 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
