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ChEMBL ligand: CHEMBL13470 (SNC-80) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | F | 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 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 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 DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay | F | 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 DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | F | 8.12 | pEC50 | 7.6 | nM | EC50 | ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376] |
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 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]GTP-gamma-S binding | F | 8.32 | pEC50 | 4.8 | nM | EC50 | J Med Chem (2006) 49: 5635-5639 [PMID:16942039] |
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 | 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 | Agonist activity at delta opioid receptor in mouse vas deferens | F | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 905-910 [PMID:16290934] |
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]