SNC80 [Ligand Id: 1611] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13470 (SNC-80)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • 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]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI F 6.2 pKd 629 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 3347-3350 [PMID:10612597]
GtoPdb - - 7.2 pKi - - - Eur J Pharmacol (1997) 326: 101-4 [PMID:9178661];
J Med Chem (1994) 37: 2125-8 [PMID:8035418]
ChEMBL Binding affinity for delta opioid receptor B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 2109-2112 [PMID:15080989]
ChEMBL Displacement of [3H]deltorphine 2 from human delta opioid receptor expressed in CHOK1 cells B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. (2008) 16: 2870-2885 [PMID:18249546]
ChEMBL Displacement of [125I]-[D-Ala2]deltorphin 2 from human cloned delta opioid receptor B 8.89 pKi 1.29 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 5994-5998 [PMID:19800791]
ChEMBL Displacement of [3H]diprenorphine from human delta opioid receptor in CHO cells B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2008) 51: 5893-5896 [PMID:18788723]
ChEMBL Displacement of [3H]-deltorphine from human delta opioid receptor expressed in CHO-K1 cells by scintillation counting analysis B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Displacement of [3H]deltrophine from human delta opioid receptor expressed in CHO-K1 cells after 120 mins by liquid scintillation counting method B 8.92 pKi 1.2 nM Ki MedChemComm (2016) 7: 317-326
ChEMBL Binding affinity was measured against mutated human Opioid receptor delta 1 (W248L) B 7.31 pIC50 49.1 nM IC50 J. Med. Chem. (1998) 41: 4767-4776 [PMID:9822547]
ChEMBL Binding affinity was measured against cloned human Opioid receptor delta 1 (wild-type,Wt) B 8.55 pIC50 2.85 nM IC50 J. Med. Chem. (1998) 41: 4767-4776 [PMID:9822547]
ChEMBL Binding inhibition of [3H]- -naltrindole (0.15 nM) to membranes in CHO cells expressing Opioid receptor delta 1 B 8.66 pIC50 2.2 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1323-1328 [PMID:10340622]
ChEMBL Inhibition of binding of [3H]- -naltrindole (0.15 nM) to membranes from CHO cells expressing Opioid receptor delta 1 B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1329-1334 [PMID:10340623]
ChEMBL Binding affinity against human opioid receptor delta 1 using [125I]-[D-Ala2]-deltorphin II as radioligand B 8.88 pIC50 1.31 nM IC50 J. Med. Chem. (2000) 43: 3878-3894 [PMID:11052793]
ChEMBL Binding affinity on cloned opioid receptor delta 1 in human HEK293S cells using [125I]-[D-Ala2]-deltorphin II as radioligand. B 8.88 pIC50 1.31 nM IC50 J. Med. Chem. (2000) 43: 3895-3905 [PMID:11052794]
ChEMBL Binding affinity for Opioid receptor delta 1 by the inhibition of binding of [3H]-p-DPDPE human cloned receptors. B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (1997) 40: 2936-2947 [PMID:9288176]
ChEMBL Agonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate F 6.12 pEC50 760 nM EC50 J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay B 6.68 pEC50 210 nM EC50 ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 7.8 pEC50 15.7 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay F 7.8 pEC50 15.7 nM EC50 Bioorg. Med. Chem. (2012) 20: 949-961 [PMID:22197670]
ChEMBL Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay B 7.84 pEC50 14.4 nM EC50 J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 8 pEC50 10 nM EC50 J. Med. Chem. (2008) 51: 5893-5896 [PMID:18788723]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay F 8.32 pEC50 4.8 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 6516-6520 [PMID:17935988]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 8.32 pEC50 4.8 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting F 8.32 pEC50 4.8 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 7340-7344 [PMID:23142613]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding F 8.32 pEC50 4.8 nM EC50 J. Med. Chem. (2006) 49: 5635-5639 [PMID:16942039]
ChEMBL Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay. F 8.44 pEC50 3.67 nM EC50 J. Med. Chem. (2000) 43: 3895-3905 [PMID:11052794]
ChEMBL Agonist potency was measured using GTP gamma-[35S] binding assay B 8.44 pEC50 3.67 nM EC50 J. Med. Chem. (2000) 43: 3878-3894 [PMID:11052793]
ChEMBL Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay F 8.52 pEC50 2.99 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5994-5998 [PMID:19800791]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding F 8.72 pEC50 1.9 nM EC50 ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
ChEMBL Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method B 8.77 pEC50 1.7 nM EC50 ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of [3H]-DPDPE from mouse DOR expressed in HEK293 cells B 7.78 pKi 16.6 nM Ki ACS Med. Chem. Lett. (2012) 3: 640-644 [PMID:23585918]
ChEMBL Binding affinity against Opioid receptor delta 1 using [3H][D-Ala2, D-Leu5]-enkephalin as radioligand B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL Binding affinity towards opioid Delta receptor using [3H]DADLE as radioligand B 8.8 pKi 1.57 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity towards opioid Delta receptor using [3H]DADLE as radioligand B 8.8 pKi 1.57 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain cerebellum membrane B 8.98 pKi 1.04 nM Ki ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
ChEMBL Displacement of [3H]DPDPE from mouse brain delta opioid receptor by scintillation counting analysis B 9.15 pKi 0.71 nM Ki Eur. J. Med. Chem. (2013) 69: 413-426 [PMID:24090913]
ChEMBL Tested for inhibition of binding of [3H]DADLE to mouse brain membranes depleted of mu binding sites by pretreatment with irreversible ligand BIT for delta opioid receptor B 5.7 pIC50 >2000 nM IC50 J. Med. Chem. (1994) 37: 2125-2128 [PMID:8035418]
ChEMBL Agonist activity was evaluated in mouse vas deferens (MVD) preparations at Opioid receptor delta 1 F 6.19 pIC50 646.8 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL In vitro antagonist activity against Opioid receptor delta 1 in the presence of 30 nM naltrindole, in a mouse vas deferens assay F 6.2 pIC50 634 nM IC50 J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL Tested for inhibition of binding of [3H]DADLE to mouse brain membranes depleted of mu binding sites by pretreatment with irreversible ligand BIT for delta opioid receptor B 7.25 pIC50 56.5 nM IC50 J. Med. Chem. (1994) 37: 2125-2128 [PMID:8035418]
ChEMBL In vitro agonist activity for Opioid receptor delta 1 was determined in a mouse vas deferens assay F 8.1 pIC50 8 nM IC50 J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum B 8.19 pIC50 6.41 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 6398-6401 [PMID:18990576]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in ICR mouse whole brain B 8.19 pIC50 6.41 nM IC50 Bioorg. Med. Chem. (2008) 16: 4304-4312 [PMID:18337104]
ChEMBL Agonist activity was evaluated in mouse vas deferens (MVD) preparations at Opioid receptor delta 1 F 8.27 pIC50 5.34 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Agonist activity using electrically induced smooth muscle contraction of mouse vas deferens. F 8.56 pIC50 2.73 nM IC50 J. Med. Chem. (1999) 42: 5455-5463 [PMID:10639287]
ChEMBL Agonist activity was evaluated in mouse vas deferens (MVD) preparations at Opioid receptor delta 1 F 8.56 pIC50 2.73 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Agonistic activity towards Opioid receptor delta 1 as inhibitory activity towards electrically stimulated mouse vas deferens F 8.57 pIC50 2.7 nM IC50 J. Med. Chem. (1996) 39: 2081-2086 [PMID:8642567]
ChEMBL Displacement of [3H]DPDPE from mouse delta opioid receptor expressed in HEK293 cells by liquid scintillation counting B 9.1 pIC50 0.8 nM IC50 Bioorg. Med. Chem. (2009) 17: 6442-6450 [PMID:19646882]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane B 8.25 pKi 5.6 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL In vitro binding affinity to Opioid receptor delta 1 in rat brain membranes by [3H]DADLE (Tyr-D-Ala-Gly-Phe-D-Leu) displacement. B 8.4 pKi 4 nM Ki J. Med. Chem. (1999) 42: 5455-5463 [PMID:10639287]
ChEMBL Displacement of [3H]DADLE from delta opioid receptor in rat brain after 60 mins by liquid scintillation counting method B 8.45 pKi 3.53 nM Ki Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512]
ChEMBL Inhibition of [3H]DPDPE radioligand binding to rat opioid receptor delta 1 site from rat brain membranes B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1109-1111 [PMID:10843229]
ChEMBL Inhibition of binding of [3H]-DPDPE to opioid receptor delta 1 from rat brain membrane. B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1741-1743 [PMID:11425550]
ChEMBL Affinity of [H]DADLE to the delta opioid receptor from rat brain B 8.8 pKi 1.57 nM Ki J. Med. Chem. (2001) 44: 972-987 [PMID:11300879]
ChEMBL Compound was evaluated for binding affinity towards Opioid receptor delta 1 by displacement of [3H]-DADLE radioligand B 8.8 pKi 1.57 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1281-1284 [PMID:10866400]
ChEMBL Inhibitory activity against Opioid receptor delta 1 in rat brain membranes using [3H]DADLE as a radioligand. B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2000) 43: 3193-3196 [PMID:10956228]
ChEMBL Displacement of [3H]DPDPE from DOR in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting method B 8.92 pKi 1.2 nM Ki J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL Inhibition of radioligand [3H]DADLE binding to rat brain Opioid receptor delta 1 B 6.37 pIC50 430 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Inhibition of [3H]- DADLE binding to Rat brain Opioid receptor delta 1 B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (1996) 39: 2081-2086 [PMID:8642567]
ChEMBL Binding affinity for Opioid receptor delta 1 by the inhibition of binding of [3H]DADAL in rat brain membranes. B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (1997) 40: 2936-2947 [PMID:9288176]
ChEMBL Inhibition of radioligand [3H]DADLE binding to rat brain Opioid receptor delta 1 B 8.54 pIC50 2.88 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Binding affinity was measured against Opioid receptor delta 1 using [3H]p-Cl-DPDPE as radioligand. B 8.97 pIC50 1.06 nM IC50 J. Med. Chem. (1998) 41: 4767-4776 [PMID:9822547]
ChEMBL Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay F 6.78 pEC50 166 nM EC50 J. Med. Chem. (2009) 52: 7724-7731 [PMID:19788201]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [125I]D-pro10-dynorphin from human cloned kappa opioid receptor B 5.38 pKi 4169 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 5994-5998 [PMID:19800791]
ChEMBL Binding affinity towards opioid kappa receptor using [3H]U-69593 as radioligand B 5.45 pKi 3535 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity towards opioid kappa receptor using [3H]U-69593 as radioligand B 5.45 pKi 3535 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Binding affinity on cloned opioid receptor kappa 1 in human HEK293S cells using [125I]-D-Pro10-dynorphin A[1-11] as radioligand. B 5.61 pIC50 2480 nM IC50 J. Med. Chem. (2000) 43: 3895-3905 [PMID:11052794]
ChEMBL Binding affinity against cloned human Opioid receptor kappa 1 using [125I]-D-Pro10-dynorphin A[1-11] as radioligand B 5.61 pIC50 2480 nM IC50 J. Med. Chem. (2000) 43: 3878-3894 [PMID:11052793]
ChEMBL Agonist activity at human kappa opioid receptor expressed in HEK293 cells by CellKey method B 5.28 pEC50 5264 nM EC50 ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL Displacement of [3H]U-69,593 from mouse brain kappa opioid receptor by scintillation counting analysis B 5.56 pKi 2750 nM Ki Eur. J. Med. Chem. (2013) 69: 413-426 [PMID:24090913]
ChEMBL Binding affinity against Opioid receptor kappa 1 using [3H]-U-69,593 as radioligand B 5.87 pKi 1348 nM Ki J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Affinity of [3H]U-69593 to opioid receptor kappa 1 from rat brain B 5.45 pKi 3535 nM Ki J. Med. Chem. (2001) 44: 972-987 [PMID:11300879]
ChEMBL Displacement of [3H]U69593 from rat kappa opioid receptor expressed in HEK293 cells by liquid scintillation counting B 5.44 pIC50 3601 nM IC50 Bioorg. Med. Chem. (2009) 17: 6442-6450 [PMID:19646882]
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 6.2 pKd 629 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL In vitro radioligand binding assay, for inhibition of [3H]U-69593 binding to Opioid receptor kappa 1, in guinea pig brain membranes. B 4.93 pKi 11700 nM Ki J. Med. Chem. (1999) 42: 5455-5463 [PMID:10639287]
ChEMBL Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes B 5.06 pKi 8760 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL Compound was evaluated for binding affinity towards Opioid receptor kappa 1 by displacement of [3H]U-69593 radioligand B 5.45 pKi 3535 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1281-1284 [PMID:10866400]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum membrane B 6 pKi >1000 nM Ki ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
ChEMBL Binding affinity for Opioid receptor kappa 1 by the inhibition of binding of [3H]U-69593 in guinea pig brain membranes. B 5.15 pIC50 7070 nM IC50 J. Med. Chem. (1997) 40: 2936-2947 [PMID:9288176]
ChEMBL Binding affinity towards Opioid receptor kappa 1 using [3H]- U-69,593 (1.5 nM) as radioligand in guinea pig brain membranes B 5.39 pIC50 4100 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1323-1328 [PMID:10340622]
ChEMBL Binding affinity towards Opioid receptor kappa 1 using [3H]- U-69,593 (1.5 nM) as radioligand in guinea pig brain membranes B 5.39 pIC50 4100 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1329-1334 [PMID:10340623]
ChEMBL Agonist activity at kappa opioid receptor in myenteric plexus muscle from guinea pig F 5.9 pIC50 1258.93 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 905-910 [PMID:16290934]
ChEMBL Inhibition of [3H]- U69,593 binding to Guinea pig Opioid receptor kappa 1 B 6 pIC50 >1000 nM IC50 J. Med. Chem. (1996) 39: 2081-2086 [PMID:8642567]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Binding affinity for mu opioid receptor B 5.89 pKi 1300 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 2109-2112 [PMID:15080989]
ChEMBL Displacement of [125I]FK33824 from human cloned mu opioid receptor B 6.45 pKi 352 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 5994-5998 [PMID:19800791]
ChEMBL Binding affinity for micro receptors by the inhibition of binding of [3H]DAMGO to Opioid receptor mu 1 in human cloned receptors. B 5.32 pIC50 4785 nM IC50 J. Med. Chem. (1997) 40: 2936-2947 [PMID:9288176]
ChEMBL Binding affinity on cloned opioid receptor mu 1 in human HEK293S cells using [125I]FK33824 as radioligand. B 6.49 pIC50 320 nM IC50 J. Med. Chem. (2000) 43: 3895-3905 [PMID:11052794]
ChEMBL Binding affinity against cloned human Opioid receptor mu 1 using [125I]FK33824 as radioligand B 6.49 pIC50 320 nM IC50 J. Med. Chem. (2000) 43: 3878-3894 [PMID:11052793]
ChEMBL Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method B 9.85 pEC50 0.14 nM EC50 ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Displacement of [3H]DAMGO from mouse brain mu opioid receptor by scintillation counting analysis B 5.62 pKi 2383 nM Ki Eur. J. Med. Chem. (2013) 69: 413-426 [PMID:24090913]
ChEMBL Binding affinity against Opioid receptor mu 1 using [3H][D-Ala2, MePhe4, Gly-ol5]-enkephalin as radioligand B 5.89 pKi 1300 nM Ki J. Med. Chem. (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain cerebellum membrane B 6.16 pKi 695 nM Ki ACS Med. Chem. Lett. (2014) 5: 368-372 [PMID:24900842]
ChEMBL Displacement of [3H]DAMGO from mouse mu opioid receptor expressed in HEK293 cells by liquid scintillation counting B 5.22 pIC50 6066 nM IC50 Bioorg. Med. Chem. (2009) 17: 6442-6450 [PMID:19646882]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane B 5.09 pKi 8070 nM Ki J. Med. Chem. (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL In vitro radioligand binding assay, for inhibition of [3H]DAMGO (Tyr-D-Ala-Gly-(Me)-Phe-Gly-ol) binding to Opioid receptor mu 1 in rat brain membranes. B 5.4 pKi 3970 nM Ki J. Med. Chem. (1999) 42: 5455-5463 [PMID:10639287]
ChEMBL Affinity of [3H]DAMGO to the mu opioid receptor from rat brain B 5.79 pKi 1614 nM Ki J. Med. Chem. (2001) 44: 972-987 [PMID:11300879]
ChEMBL Compound was evaluated for binding affinity towards Opioid receptor mu 1 by displacement of [3H]-DAMGO radioligand B 5.79 pKi 1614 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1281-1284 [PMID:10866400]
ChEMBL Binding affinity towards opioid Mu receptor using [3H]DAMGO as radioligand B 5.79 pKi 1614 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Binding affinity towards opioid Mu receptor using [3H]DAMGO as radioligand B 5.79 pKi 1614 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity by inhibition of [3H]DAMGO binding to Opioid receptor mu 1 from rat brain membranes B 5.89 pKi 1300 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1109-1111 [PMID:10843229]
ChEMBL Inhibition of binding of [3H]DAMGO to opioid receptor mu 1 from rat brain membrane. B 5.89 pKi 1300 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1741-1743 [PMID:11425550]
ChEMBL Inhibition of radioligand [3H]DAMGO binding to rat brain Opioid receptor mu 1 using 100 nM DAMGO B 5.03 pIC50 9366 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Evaluated for inhibition of [3H]DAMGO binding from mu receptor in rat brain membranes B 5.03 pIC50 9366 nM IC50 J. Med. Chem. (1994) 37: 2125-2128 [PMID:8035418]
ChEMBL Evaluated for inhibition of [3H]DAMGO binding from mu receptor in rat brain membranes B 5.24 pIC50 5712 nM IC50 J. Med. Chem. (1994) 37: 2125-2128 [PMID:8035418]
ChEMBL Binding affinity towards mu opioid receptor using [3H]- -DAMGO (1.5 nM) as radioligand in rat brain membranes B 5.32 pIC50 4800 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1329-1334 [PMID:10340623]
ChEMBL Binding affinity towards mu opioid receptor using [3H]- -DAMGO (1.5 nM) as radioligand in rat brain membranes B 5.32 pIC50 4800 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1323-1328 [PMID:10340622]
ChEMBL Binding affinity was measured against Opioid receptor mu 1 using [3H]-DAMGO as radioligand. B 5.6 pIC50 2500 nM IC50 J. Med. Chem. (1998) 41: 4767-4776 [PMID:9822547]
ChEMBL Binding affinity for Opioid receptor mu 1 by the inhibition of binding of [3H]DAMGO in rat brain membranes. B 5.61 pIC50 2467 nM IC50 J. Med. Chem. (1997) 40: 2936-2947 [PMID:9288176]
ChEMBL Inhibition of radioligand [3H]DAMGO binding to rat brain Opioid receptor mu 1 using 100 nM DAMGO B 5.61 pIC50 2467 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Inhibition of [3H]- DAMGO binding to Rat brain Opioid receptor mu 1 B 5.61 pIC50 2467 nM IC50 J. Med. Chem. (1996) 39: 2081-2086 [PMID:8642567]
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 blocked with 6000 nM CTAP F 6.17 pKd 673 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 blocked with 6000 nM CTAP F 6.17 pKd 673 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition F 6.5 pKd 317 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 6.5 pKd 317 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Agonist activity at mu opioid receptor in myenteric plexus muscle from guinea pig F 5 pIC50 <10000 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 905-910 [PMID:16290934]
ChEMBL Agonistic activity for Opioid receptor mu 1 as inhibitory activity towards electrically stimulated guinea pig ileum F 5.26 pIC50 5457 nM IC50 J. Med. Chem. (1996) 39: 2081-2086 [PMID:8642567]
ChEMBL Agonist activity was evaluated in guinea pig ileum (GPI) preparations at Opioid receptor mu 1 F 5.26 pIC50 5457 nM IC50 J. Med. Chem. (1997) 40: 695-704 [PMID:9057856]
ChEMBL Agonist activity using strips of guinea pig ileum longitudinal muscle myenteric plexus. F 5.26 pIC50 5450 nM IC50 J. Med. Chem. (1999) 42: 5455-5463 [PMID:10639287]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.6 pIC50 2511.89 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.6 pIC50 2511.89 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]