[3H]naloxone [Ligand Id: 1676] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL80 (Dbl naloxone, Nalone, Naloxona, Naloxone, Narcan, Narcanti, NSC-70413, Suboxone)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • CCR5/C-C chemokine receptor type 5 in Mouse [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682]
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  • cytochrome b-245 beta chain/Cytochrome b-245 heavy chain in Human [ChEMBL: CHEMBL1287627] [GtoPdb: 3002] [UniProtKB: P04839]
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  • 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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  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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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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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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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 4.3 pKi >50000 nM Ki Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950]
CCR5/C-C chemokine receptor type 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682]
ChEMBL Binding affinity to CCR5 in C57BL/6J mouse brain membrane B 7.68 pKd 20.8 nM Kd Proc Natl Acad Sci U S A (2007) 104: 6061-6065 [PMID:17389363]
ChEMBL Binding affinity to CCR5 in NY1DD transgenic mouse brain membrane B 7.98 pKd 10.5 nM Kd Proc Natl Acad Sci U S A (2007) 104: 6061-6065 [PMID:17389363]
cytochrome b-245 beta chain/Cytochrome b-245 heavy chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287627] [GtoPdb: 3002] [UniProtKB: P04839]
ChEMBL Inhibition of human NOX2 expressed in HEK293T cells assessed as inhibition of LPS-induced superoxide production pre-incubated for 45 mins and measure after 10 mins by chemiluminescence based analysis B 5.71 pIC50 1960 nM IC50 J Med Chem (2023) 66: 11632-11655 [PMID:37650225]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.7 pIC50 2000 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]DPDPE from human DOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 5.82 pKi 1516 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 6.29 pKi 515 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Displacement of [3H]diprenorphine human delta opioid receptor expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method B 6.92 pKi 120 nM Ki ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376]
ChEMBL Displacement of [3H]deltrophine from human delta opioid receptor expressed in CHO-K1 cells after 120 mins by liquid scintillation counting method B 6.99 pKi 103 nM Ki Medchemcomm (2016) 7: 317-326
ChEMBL Displacement of [3H]-deltorphine from human delta opioid receptor expressed in CHO-K1 cells by scintillation counting analysis B 6.99 pKi 103 nM Ki J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Displacement of [3H]-diprenorphine from human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by competition radioligand binding assay B 7.01 pKi 98.1 nM Ki J Med Chem (2020) 63: 7663-7694 [PMID:32530286]
ChEMBL Displacement of [3H]naltrindole from human opioid delta receptor expressed in CHO cells B 7.12 pKi 76 nM Ki J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL Displacement of [3H]-diprenorphine from human DOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method B 7.14 pKi 72.8 nM Ki J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL Displacement of [3H]-diprenorphine from human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method B 7.15 pKi 70 nM Ki ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL Displacement of [125I]OXY from human delta opioid receptor expressed in CHO cells B 7.29 pKi 51 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor B 7.37 pKi 42.6 nM Ki J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 in CHO cells B 7.39 pKi 41 nM Ki Bioorg Med Chem Lett (2000) 10: 523-526 [PMID:10741545]
ChEMBL Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cells after 3 hrs by scintillation counting B 7.42 pKi 38 nM Ki Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
ChEMBL In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement. B 7.43 pKi 37 nM Ki J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Concentration required to inhibit the binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human delta opioid receptor B 7.48 pKi 33 nM Ki Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL Displacement of [3H]diprenorphine from human cloned delta opioid receptor B 7.48 pKi 33 nM Ki Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells B 7.48 pKi 33 nM Ki J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells B 7.48 pKi 33 nM Ki J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor (unknown origin) transfected into HEK293 cells by microplate scintillation counting B 7.52 pKi 30 nM Ki J Nat Prod (2015) 78: 1461-1465 [PMID:26035635]
ChEMBL Displacement of [3H]DPN from human recombinant delta-type opioid receptor expressed in CHO cell membranes B 7.67 pKi 21.38 nM Ki Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]
ChEMBL In vivo binding affinity against delta Opioid receptor was measured by using labeled ligand [3H]DADLE (1 nM) with 4 nM sufentanil B 7.72 pKi 19 nM Ki J Med Chem (1994) 37: 3121-3127 [PMID:7932535]
ChEMBL Binding affinity to delta-opioid receptor (unknown origin) B 7.8 pKi 15.85 nM Ki J Nat Prod (2021) 84: 713-723 [PMID:32870011]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.84 pIC50 1461 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr F 6.82 pIC50 153 nM IC50 J Med Chem (2020) 63: 7663-7694 [PMID:32530286]
ChEMBL Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand B 6.82 pIC50 151 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr F 6.84 pIC50 146 nM IC50 ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membrane B 6.86 pIC50 138 nM IC50 J Nat Prod (2007) 70: 866-868 [PMID:17388627]
ChEMBL Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells B 6.86 pIC50 138 nM IC50 J Nat Prod (2007) 70: 1946-1950 [PMID:18039010]
ChEMBL Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK293 cells B 6.86 pIC50 138 nM IC50 J Nat Prod (2006) 69: 1295-1299 [PMID:16989522]
ChEMBL Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membranes B 6.86 pIC50 138 nM IC50 J Nat Prod (2007) 70: 872-875 [PMID:17451272]
ChEMBL Antagonist activity at human DOR expressed in CHO cell membranes assessed as reduction in SNC80-induced response incubated for 1 hr by [35S]-GTPgammaS coupling assay F 7.11 pIC50 78.2 nM IC50 J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane B 7.21 pIC50 62 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL Inhibition of [3H]DPDPE binding to guinea pig brain membrane Opioid receptor delta 1 at 1.0 nM B 7.21 pIC50 62 nM IC50 J Med Chem (1992) 35: 2374-2384 [PMID:1320121]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Tested for inhibitory activity against (DPDE)delta receptor in mouse vas deferens B 7.3 pKd 50.12 nM Kd J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL Antagonist activity at delta opioid receptor in Swiss mouse vas deferens assessed as reversal of DSLET effect on electrically-induced driven twitch F 7.35 pKd 44.67 nM Kd Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Affinity against the Opioid receptor delta 1 B 7.74 pKd 18 nM Kd J Med Chem (1986) 29: 531-537 [PMID:3007760]
ChEMBL Displacement of [3H]DPDPE from DOR in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting method B 6.99 pKi 103 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 6.99 pKi 103 nM Ki Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825]
ChEMBL Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates B 7.49 pKi 32 nM Ki J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
ChEMBL Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting B 8.6 pKi 2.5 nM Ki Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting analysis B 8.62 pKi 2.4 nM Ki Medchemcomm (2016) 7: 2368-2380
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in rat membranes after 120 mins by scintillation counting analysis B 8.62 pKi 2.4 nM Ki J Med Chem (2019) 62: 4204-4217 [PMID:30939014]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 4.7 pKi >20000 nM Ki J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U-69593 from human KOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 6.44 pKi 362 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 7.52 pKi 30 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to kappa-opioid receptor (unknown origin) B 7.8 pKi 15.85 nM Ki J Nat Prod (2021) 84: 713-723 [PMID:32870011]
ChEMBL Displacement of [3H]Cl-977 from human kappa opioid receptor expressed on HEK-293 cells by liquid scintillation counting method B 7.82 pKi 15 nM Ki Medchemcomm (2016) 7: 317-326
ChEMBL Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells B 7.83 pKi 14.7 nM Ki J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement. B 7.97 pKi 10.7 nM Ki J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Displacement of [3H]diprenorphine from human cloned kappa opioid receptor B 8.04 pKi 9.2 nM Ki Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL Binding affinity at cloned human kappa opioid receptor by [3H]diprenorphine displacement. B 8.04 pKi 9.2 nM Ki Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells B 8.04 pKi 9.2 nM Ki J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells B 8.04 pKi 9.2 nM Ki J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL Displacement of [3H]DPN from human recombinant kappa-type opioid receptor expressed in CHO cell membranes B 8.35 pKi 4.47 nM Ki Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]
ChEMBL Displacement of [125I]OXY from human kappa opioid receptor expressed in CHO cells B 8.52 pKi 3 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 expressed in HEK 293 cells B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2000) 10: 523-526 [PMID:10741545]
ChEMBL Displacement of [3H]U-69593 from human opioid kappa receptor expressed in CHO cells B 8.96 pKi 1.1 nM Ki J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL Displacement of [3H]U69563 from human kappa-opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 9.6 pKi 0.25 nM Ki Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
ChEMBL Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding F 6.49 pIC50 320 nM IC50 J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL Antagonist activity at human KOR expressed in CHO cell membranes assessed as reduction in U50,488 induced response incubated for 1 hr by liquid scintillation counting based [35S]GTP-gamma-S assay B 6.85 pIC50 140 nM IC50 J Med Chem (2016) 59: 10291-10298 [PMID:27797517]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 7.12 pIC50 75 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488 F 7.3 pIC50 49.8 nM IC50 J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand B 8.82 pIC50 1.5 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 8 pEC50 10 nM EC50 J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL Effective concentration for half-maximal stimulation was determined by [35S]GTP-gamma-S, assay F 8.18 pEC50 6.6 nM EC50 J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL Antagonist activity at kappa opioid receptor in Swiss mouse vas deferens assessed as reversal of U50488 effect on electrically-induced driven twitch F 6.9 pKd 125.89 nM Kd Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor kappa 1 B 8.35 pKd 4.5 nM Kd Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696]
ChEMBL Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa) B 9 pKd 1 nM Kd J Med Chem (1986) 29: 531-537 [PMID:3007760]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Tested for its antagonist activity against kappa receptor using U-69,593 as radioligand in isolated guinea pig ileum F 7.7 pKd 19.95 nM Kd J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue B 7.18 pKi 66 nM Ki J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
ChEMBL Binding affinity towards kappa-opioid receptor by displacement of [3H]-EKC at from guinea pig cortical tissue B 7.18 pKi 66 nM Ki J Med Chem (1993) 36: 2833-2841 [PMID:8410998]
ChEMBL Tested for binding affinity towards kappa receptor in presence of [3H]EKC radioligand B 7.18 pKi 66 nM Ki J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL Displacement of [3H]Cl-977 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis B 7.82 pKi 15 nM Ki J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL In vivo binding affinity against kappa opioid receptor was measured by using labeled ligand [3H]ethylketocyclazocine (1 nM) with 500 nM DADLE and 20 nM sufentanil B 7.92 pKi 12 nM Ki J Med Chem (1994) 37: 3121-3127 [PMID:7932535]
ChEMBL Displacement of [3H]U-69,593 from kappa-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting B 8.14 pKi 7.3 nM Ki J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting B 8.14 pKi 7.3 nM Ki J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL Displacement of [3H]U-69,593 from KOR in guinea pig brain membranes after 120 mins by scintillation counting method B 8.14 pKi 7.3 nM Ki J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis B 8.14 pKi 7.3 nM Ki J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Displacement of [3H]-U69593 from KOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay B 8.14 pKi 7.3 nM Ki Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes after 150 mins by scintillation counting B 8.14 pKi 7.3 nM Ki Eur J Med Chem (2011) 46: 1972-1982 [PMID:21481987]
ChEMBL Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794]
ChEMBL Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane B 8.16 pKi 6.9 nM Ki Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.16 pKi 6.9 nM Ki Medchemcomm (2016) 7: 2368-2380
ChEMBL Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting analysis B 8.16 pKi 6.9 nM Ki J Med Chem (2019) 62: 4204-4217 [PMID:30939014]
ChEMBL Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes B 8.49 pKi 3.2 nM Ki J Med Chem (2001) 44: 2814-2826 [PMID:11495592]
ChEMBL Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane B 8.5 pKi 3.17 nM Ki Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membarnes by liquid scintillation counting method B 8.51 pKi 3.1 nM Ki Medchemcomm (2016) 7: 317-326
ChEMBL Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane B 7.3 pIC50 50 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL Displacement of 0.5 nM [3H]bremazocine from guinea pig brain membrane opioid receptor kappa with 100 nM DAGO and 100 nM DPDPE B 7.3 pIC50 50 nM IC50 J Med Chem (1992) 35: 2374-2384 [PMID:1320121]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Antagonist activity against mu opioid receptor assessed as effect on endomorphin-2-induced calcium response in CHO cells by aequorin luminescence based calcium assay F 9.66 pKd 0.22 nM Kd J Med Chem (2007) 50: 512-520 [PMID:17266203]
ChEMBL Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay F 9.66 pKd 0.22 nM Kd Bioorg Med Chem Lett (2008) 18: 1350-1353 [PMID:18207400]
ChEMBL Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 6.45 pKi 354 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL Displacement of [3H]-diprenorphine from human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by competition radioligand binding assay B 7.23 pKi 59.5 nM Ki J Med Chem (2020) 63: 7663-7694 [PMID:32530286]
ChEMBL Displacement of [3H]-diprenorphine from human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method B 7.29 pKi 51.2 nM Ki ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL Displacement of [3H]-diprenorphine from human MOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method B 7.29 pKi 51 nM Ki J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL Displacement of [3H]diprenorphine human MOR expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method B 7.37 pKi 43 nM Ki ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 8.09 pKi 8.06 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells B 8.37 pKi 4.23 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells B 8.43 pKi 3.7 nM Ki J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells B 8.43 pKi 3.7 nM Ki J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL Inhibition of binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human mu opioid receptor B 8.43 pKi 3.7 nM Ki Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL Displacement of [3H]diprenorphine from human cloned mu opioid receptor B 8.43 pKi 3.7 nM Ki Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement. B 8.44 pKi 3.63 nM Ki J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO-K1 cells by scintillation counting analysis B 8.64 pKi 2.3 nM Ki J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Displacement of [3H]naloxone from human mu opioid receptor expressed in CHO-K1 cells after 150 mins by liquid scintillation counting method B 8.64 pKi 2.3 nM Ki Medchemcomm (2016) 7: 317-326
ChEMBL Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells B 8.64 pKi 2.27 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [3H]DAGO from mu opioid receptor B 8.8 pKi 1.6 nM Ki J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL Binding affinity to mu opioid receptor B 8.82 pKi 1.5 nM Ki Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950]
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 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 8.94 pKi 1.15 nM Ki J Med Chem (2015) 58: 9754-9767 [PMID:26632862]
ChEMBL Binding affinity to mu-opioid receptor (unknown origin) B 9 pKi 1 nM Ki J Nat Prod (2021) 84: 713-723 [PMID:32870011]
ChEMBL Displacement of [125I]OXY from human mu opioid receptor expressed in CHO cells B 9.01 pKi 0.98 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells B 9.1 pKi 0.79 nM Ki J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 9.18 pKi 0.66 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells B 9.24 pKi 0.57 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [3H]DPN from human recombinant mu-type opioid receptor expressed in CHO cell membranes B 9.25 pKi 0.56 nM Ki Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]
ChEMBL Displacement of [3H]DAMGO from human mu-opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 9.64 pKi 0.23 nM Ki Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
ChEMBL Negative allosteric modulation of human mu opioid receptor expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of fentanyl F 6.14 pIC50 722 nM IC50 J Med Chem (2023) 66: 9466-9494 [PMID:37437224]
ChEMBL Antagonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay F 6.52 pIC50 302 nM IC50 J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay F 7.02 pIC50 94.84 nM IC50 J Med Chem (2017) 60: 6733-6750 [PMID:28726402]
ChEMBL Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay F 7.35 pIC50 45 nM IC50 J Med Chem (2017) 60: 6733-6750 [PMID:28726402]
ChEMBL Antagonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in fentanyl induced cAMP production incubated for 30 mins by Lance ultra cAMP assay F 7.57 pIC50 27 nM IC50 RSC Med Chem (2022) 13: 175-182 [PMID:35308026]
ChEMBL Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as inhibition of DAGO-stimulated [35S]GTPgammaS binding F 7.64 pIC50 23 nM IC50 J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 7.7 pIC50 20 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonist activity at human cloned mu opioid receptor assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding F 8.14 pIC50 7.3 nM IC50 Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL Antagonist activity against human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding F 8.14 pIC50 7.3 nM IC50 J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells F 8.14 pIC50 7.3 nM IC50 J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL Concentration required to inhibit agonist (loperamide) stimulated [35S]GTP-gamma-S, binding to membranes containing the cloned human mu opioid receptor F 8.14 pIC50 7.3 nM IC50 Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand B 8.7 pIC50 2 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL Displacement of radiolabeled DAMGO from human recombinant mu opioid receptor expressed in OPRM1 cells B 8.73 pIC50 1.87 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
Mu opioid receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3041] [UniProtKB: P79350]
ChEMBL Inhibition of 0.5 nM [3H]- Bremazocine binding to Opioid receptor mu 1 of bovine striatum membrane B 8.3 pIC50 5 nM IC50 J Med Chem (1990) 33: 2286-2296 [PMID:2165166]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Antagonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as reversal of Sufentanil effect on electrically-induced driven twitch F 7.99 pKd 10.23 nM Kd Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026]
ChEMBL Antagonist activity at mouse mu opioid receptor expressed in CHO cells cotransfected with Galphaqi5 assessed as inhibition of DAMGO-induced increase in intracellular calcium concentration preincubated for 60 mins in Fluo4AM solution followed by compound addition and further incubated for 15 mins followed by DAMGO stimulation by Fluo4AM dye based assay F 7.81 pIC50 15.37 nM IC50 J Med Chem (2019) 62: 11399-11415 [PMID:31782922]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Opioid receptor mu 2 affinity against the receptor site model site 2(mu2) B 8.3 pKd 5 nM Kd J Med Chem (1986) 29: 531-537 [PMID:3007760]
ChEMBL Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor mu 1 B 8.52 pKd 3 nM Kd Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696]
GtoPdb CHO and BHK cell lines stably expressing the rat μ receptor - 9 pKd 1 nM Kd Mol Pharmacol (1996) 50: 1214-22 [PMID:8913353]
ChEMBL Opioid receptor mu 1 affinity against the receptor site model site 1 (mu1) B 9.4 pKd 0.4 nM Kd J Med Chem (1986) 29: 531-537 [PMID:3007760]
ChEMBL Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates B 8.2 pKi 6.3 nM Ki J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
ChEMBL Binding affinity towards mu opioid receptor by displacement of [3H]NAL from rat brain homogenates B 8.43 pKi 3.7 nM Ki J Med Chem (1993) 36: 2833-2841 [PMID:8410998]
ChEMBL Tested for binding affinity towards mu receptor in presence of [3H]NAL radioligand B 8.43 pKi 3.7 nM Ki J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL Displacement of [3H]-naloxone from rat mu opioid receptor expressed in HEK cells after 60 mins B 8.7 pKi 2 nM Ki Bioorg Med Chem (2014) 22: 4694-4703 [PMID:25087049]
ChEMBL Inhibition of [3H]DAMGO binding to rat Opioid receptor mu 1 B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2000) 10: 523-526 [PMID:10741545]
ChEMBL Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. B 8.97 pKi 1.07 nM Ki J Med Chem (1989) 32: 663-671 [PMID:2563773]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Tested for its antagonist activity against mu receptor using DAMGO as radioligand in isolated guinea pig ileum F 8.5 pKd 3.16 nM Kd J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL Negative logarithm of the molar concentration of Opioid receptor mu 1 was determined in guinea pig ileum B 8.73 pKd 1.86 nM Kd Bioorg Med Chem Lett (2000) 10: 2745-2748 [PMID:11133082]
ChEMBL Displacement of [3H]-DAMGO from MOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay B 8.64 pKi 2.3 nM Ki Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825]
ChEMBL Displacement of [3H]DAMGO from mu-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting B 8.64 pKi 2.3 nM Ki J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
ChEMBL Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting B 8.68 pKi 2.1 nM Ki Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.68 pKi 2.1 nM Ki Medchemcomm (2016) 7: 2368-2380
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.68 pKi 2.1 nM Ki J Med Chem (2019) 62: 4204-4217 [PMID:30939014]
ChEMBL In vivo binding affinity against mu opioid receptor was measured by using labeled ligand [3H]naloxone (0.5 nM) B 8.96 pKi 1.1 nM Ki J Med Chem (1994) 37: 3121-3127 [PMID:7932535]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membrane B 9.17 pKi 0.68 nM Ki Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073]
ChEMBL Affinity to mu-receptor, using [3H]DAMGO as radioligand in homogenates of guinea pig brain membranes B 9.17 pKi 0.68 nM Ki J Med Chem (2001) 44: 2814-2826 [PMID:11495592]
ChEMBL Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane B 8.05 pIC50 8.9 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL inhibition of 1.0 nM [3H]- DAGO binding to guinea pig brain membrane opioid receptor mu B 8.05 pIC50 8.9 nM IC50 J Med Chem (1992) 35: 2374-2384 [PMID:1320121]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL In vivo binding affinity against sigma Opioid receptor was measured by using labeled ligand [3H]-SKF- 10,047 (1 nM) B 4 pKi >100000 nM Ki J Med Chem (1994) 37: 3121-3127 [PMID:7932535]
ChEMBL Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain homogenate B 5 pKi >10000 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]

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]