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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL38874 (DAMGO)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
There should be some charts here, you may need to enable JavaScript!
  • CCK2 receptor/Cholecystokinin B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
There should be some charts here, you may need to enable JavaScript!
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
There should be some charts here, you may need to enable JavaScript!
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
There should be some charts here, you may need to enable JavaScript!
  • NK1 receptor/Neurokinin 1 receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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 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 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 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 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 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 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 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 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 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 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 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 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 B 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 B 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 B 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 B 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 B 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 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 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 B 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