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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 | Displacement of [3H]-DPDPE from DOR in rat brain membranes measured by competitive radioligand receptor binding assay | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825] |
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 34:
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]