DAMGO [Ligand Id: 1647] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL38874
  • A1 receptor/Adenosine receptor A1 in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta-type opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta-type opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • CCK2 receptor/Gastrin/cholecystokinin type B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa-type opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa-type opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu-type opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu-type opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu-type opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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  • NK1 receptor/Substance-P receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine receptor A1 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]
δ receptor/Delta-type 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 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 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 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]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]-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 Radioligand Binding Assay: Each compound was initially tested at 20 μM and was incubated with 3H-DPN at a concentration equal to the Kd (0.4 nM) of the radioligand in μOR containing Sf9 insect cell membranes. The reaction contained 40 fmol of μOR and was incubated in a buffer of 20 mM HEPES pH 7.5, 100 mM sodium chloride, and 0.1% bovine serum albumin for 1 hour at 25° C. To separate free from bound radioligand, reactions were rapidly filtered over Whatman GF/B filters with the aid of a Brandel harvester and 3H-DPN counts were measured by liquid scintillation. Compounds with more than 25% of 3H-DPN radioactivity were further tested in full dose-response to determine the affinity (Ki) in HEK293 membranes. Subsequently, the 15 analogs were tested in full dose-response for affinity at the μOR and the κOR by the National Institutes of Mental Health Psychoactive Drug Screen Program (PDSP), as were the affinities of compounds 12, PZM21, and their stereoisomers at the μOR, δOR, κOR and nociception receptor. B 6.01 pKi 980 nM Ki US-11484525-B2. Mu opioid receptor modulators (2022)
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-type 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-type 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]
CCK2 receptor/Gastrin/cholecystokinin type 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]
κ receptor/Kappa-type 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 Radioligand Binding Assay: Each compound was initially tested at 20 μM and was incubated with 3H-DPN at a concentration equal to the Kd (0.4 nM) of the radioligand in μOR containing Sf9 insect cell membranes. The reaction contained 40 fmol of μOR and was incubated in a buffer of 20 mM HEPES pH 7.5, 100 mM sodium chloride, and 0.1% bovine serum albumin for 1 hour at 25° C. To separate free from bound radioligand, reactions were rapidly filtered over Whatman GF/B filters with the aid of a Brandel harvester and 3H-DPN counts were measured by liquid scintillation. Compounds with more than 25% of 3H-DPN radioactivity were further tested in full dose-response to determine the affinity (Ki) in HEK293 membranes. Subsequently, the 15 analogs were tested in full dose-response for affinity at the μOR and the κOR by the National Institutes of Mental Health Psychoactive Drug Screen Program (PDSP), as were the affinities of compounds 12, PZM21, and their stereoisomers at the μOR, δOR, κOR and nociception receptor. B 5.48 pKi 3300 nM Ki US-11484525-B2. Mu opioid receptor modulators (2022)
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-type 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-type 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-type 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 Radioligand Binding Assay: Each compound was initially tested at 20 μM and was incubated with 3H-DPN at a concentration equal to the Kd (0.4 nM) of the radioligand in μOR containing Sf9 insect cell membranes. The reaction contained 40 fmol of μOR and was incubated in a buffer of 20 mM HEPES pH 7.5, 100 mM sodium chloride, and 0.1% bovine serum albumin for 1 hour at 25° C. To separate free from bound radioligand, reactions were rapidly filtered over Whatman GF/B filters with the aid of a Brandel harvester and 3H-DPN counts were measured by liquid scintillation. Compounds with more than 25% of 3H-DPN radioactivity were further tested in full dose-response to determine the affinity (Ki) in HEK293 membranes. Subsequently, the 15 analogs were tested in full dose-response for affinity at the μOR and the κOR by the National Institutes of Mental Health Psychoactive Drug Screen Program (PDSP), as were the affinities of compounds 12, PZM21, and their stereoisomers at the μOR, δOR, κOR and nociception receptor. B 7.6 pKi 25 nM Ki US-11484525-B2. Mu opioid receptor modulators (2022)
ChEMBL Displacement of [3H]-diprenorphine from recombinant human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition constant incubated for 60 mins by scintillation counter analysis B 7.78 pKi 16.5 nM Ki J Med Chem (2024) 67: 10447-10463 [PMID:38869493]
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 MOR expressed in CHO-K1 cell membranes incubated for 90 mins measured by MicroBeta scintillation counter method B 8.49 pKi 3.2 nM Ki Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067]
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 MOR (unknown origin) B 8.82 pKi 1.52 nM Ki Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
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 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 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 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 Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay B 8.83 pKi 1.49 nM Ki Bioorg Med Chem Lett (2022) 72: 128860-128860 [PMID:35724925]
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 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 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 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 (unknown origin) B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) assessed as inhibition constant incubated for 180 mins by competitive radioligand binding assay B 9.05 pKi 0.9 nM Ki J Med Chem (2023) 66: 3312-3326 [PMID:36827198]
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) assessed as inhibition constant incubated for 180 mins by competitive radioligand binding assay B 9.1 pKi 0.79 nM Ki J Med Chem (2023) 66: 3312-3326 [PMID:36827198]
ChEMBL Binding affinity to MOP (unknown origin) assessed as inhibition constant B 9.16 pKi 0.69 nM Ki ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908]
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 Inhibition of MOP (unknown origin) B 8.74 pIC50 1.8 nM IC50 ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908]
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 Opioid Receptor Binding Assay: The measurement of opioid receptor binding affinity was conducted using a radioligand binding assay on the membranes prepared from HEK293 cells (human embryonic kidney cell line) that were heterologously expressed for the recombinant human mu, delta or kappa opioid receptors.The assay buffers used for opioid receptor binding studies were 50 mM Tris.HCl (pH 7.4) for KOR, 50 mM Tris.HCl (pH 7.4) with 5 mM MgCl2 for MOR, and 50 mM Tris.HCl (pH 7.4) with 10 mM MgCl2 plus 1 mM EDTA for DOR. The wash buffer solution contained 50 mM Tris.HCl with pH 7.4.The opioid receptor binding affinity were compared to three known standards: Naltrindole, U-50488 (trans-(+)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]phenylacetamide, see M. Doi, T. Ishida and M, Inoue; Structure of K-agonist, U-50488 Acta Cryst. (1990). C46, 676-678), and DAMGO (D-Ala2 MePhe4,Gly(ol)5]encephalin, see Allan D. Blake, George Bot, John C. Freeman, and Terry Reisine‡ Differential Opioid Agonist Regulation of the Mouse m Opioid Receptor* THE JOURNAL OF BIOLOGICAL CHEMISTRY Vol. 272, No. 2, Issue of January 10, pp. 782-790, 1997).The radio ligands were prepared at the final concentration of 0.5 nM for [3H]DAMGO, 0.5 nM for [3H]diprenorphine, and 0.5 nM for [3H] DADLE, which were used as the competing radioligands for mu, kappa and delta receptor respectively.Cell membrane of HEK293 cells transfected with opioid receptors was prepared in the amount of 20 ug of MOR, 6.7 ug of KOR and 6.7 ug of DOR per each well respectively. These membranes containing the receptor of interest were incubated with increasing concentrations of test compound in the presence of a single concentration of radioligand. The fixed concentration of the radioligand was used and serial dilutions of the test compound were prepared.Testing started at 10 uM of testing compound to 4-fold serial dilution for 8-points detection. 1 μl of compounds/high control/low control was transferred in to the 96 well plates according to the plate map, and then 100 μl of membrane stock solution was dispensed into the plate followed by 100 μl of radio ligand solution. The well plated were incubated for 1 hour at room temperature with 300 rpm gentle agitation. Then, soaked the Unifilter-96 GF/C filter plates with 50 μl of 0.3% Poly ethyleneimine per well for at least 0.5 hour at room temperature, and filtered the reaction mixture through the plates using FilterMate™harvester, then wash each plate for four times with cold wash buffer. The filter plates are then dried for 1 hour at 50° C. After drying, the filter was sealed in polyethylene and adds 50 μl of Perkin Elmer Microscint 20 cocktail and the radioactivity counted in a Perkin Elmer MicroBeta2 counter.Specific binding is determined by subtraction of the Bound CPM values in the presence of 50-100× excess of cold ligand. Data is fitted using the saturation analysis non-linear curve fitting routines in Prism®. Calculation of the inhibition was conducted using following equation: % Inhibition=(1−(Assay well−Average_LC)/(Average_HC−Average_LC))*100%Binding data was analyzed using GraphPad Prism 5.0 and IC50 data was generated by non-linear regression from dose response curves. Use the model “log (inhibitor) vs. response—Variable slope” was used to fit the data. B 9.53 pIC50 0.29 nM IC50 US-11492374-B2. Peptides for treatment of medical disorders (2022)
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 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 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 MOR expressed in CHO-K1 cells assessed as decrease in beta-arrestin 2 recruitment incubated for 90 mins by HitHunter cAMP analysis F 7.03 pEC50 93.2 nM EC50 J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
ChEMBL Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay F 7.19 pEC50 64.9 nM EC50 J Med Chem (2023) 66: 17138-17154 [PMID:38095323]
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 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 [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 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 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 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 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 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 Agonist activity at human MOR expressed in CHO-K1 cells co-expressing G-alpha15 by calcium mobilization assay F 7.43 pEC50 36.8 nM EC50 J Med Chem (2024) 67: 272-288 [PMID:38118143]
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 mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting analysis F 7.79 pEC50 16.1 nM EC50 Eur J Med Chem (2023) 258: 115589-115589 [PMID:37413884]
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 MOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis B 8.09 pEC50 8.1 nM EC50 J Med Chem (2021) 64: 9458-9483 [PMID:34152138]
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 MOR (unknown origin) by Glo sensor assay F 8.35 pEC50 4.43 nM EC50 Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
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 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 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 Displacement of [3H]-DAMGO from MOR (unknown origin) B 8.69 pEC50 2.06 nM EC50 Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
ChEMBL Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 45 mins by cAMP HTRF assay F 8.7 pEC50 2 nM EC50 Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067]
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 CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis F 9.48 pEC50 0.33 nM EC50 J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
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]
ChEMBL Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay F 9.68 pEC50 0.21 nM EC50 Eur J Med Chem (2022) 243: 114728-114728 [PMID:36084534]
μ receptor/Mu-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Displacement of [3H] DAMGO from mouse MOR expressed in CHO cell membrane incubated for 90 mins by scintillation method B 8.64 pKi 2.3 nM Ki J Med Chem (2021) 64: 9458-9483 [PMID:34152138]
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 Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay F 6.61 pEC50 248 nM EC50 J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
ChEMBL 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 6.61 pEC50 245.47 nM EC50 J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
ChEMBL Agonist activity at mouse MOR expressed in CHO cells incubated for 15 mins by calcium mobilization assay F 7.16 pEC50 68.4 nM EC50 J Med Chem (2024) 67: 603-619 [PMID:38156970]
ChEMBL 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 7.26 pEC50 54.95 nM EC50 J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
ChEMBL 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 7.26 pEC50 54.4 nM EC50 J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
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 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 HA-tagged mouse mu opioid receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by Glo Sensor assay B 8.15 pEC50 7 nM EC50 J Med Chem (2023) 66: 3312-3326 [PMID:36827198]
ChEMBL Agonist activity at HA-tagged mouse mu opioid receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by Glo Sensor assay B 8.2 pEC50 6.31 nM EC50 J Med Chem (2023) 66: 3312-3326 [PMID:36827198]
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]
ChEMBL 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 8.48 pEC50 3.31 nM EC50 J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
ChEMBL 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 8.48 pEC50 3.28 nM EC50 J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
μ receptor/Mu-type 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]
ChEMBL Displacement of [3H] DAMGO from rat mu-opioid receptor extracted from CHO cell membrane assessed as inhibition constant by liquid scintillation counting analysis B 8.64 pKi 2.3 nM Ki Eur J Med Chem (2024) 276: 116643-116643 [PMID:38986343]
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 Displacement of [3H]-DAMGO from Sprague-Dawley rat brain membrane mu opioid receptor incubated for 45 mins by liquid scintillation counting analysis B 8.83 pKi 1.49 nM Ki Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113]
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 Inhibition of MOR in rat brain membrane by liquid scintillation counter analysis B 8.94 pKi 1.16 nM Ki Eur J Med Chem (2023) 260: 115783-115783 [PMID:37678143]
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-type 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]
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]
NK1 receptor/Substance-P 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]

ChEMBL data shown on this page come from version 36:

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]