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

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ChEMBL ligand: CHEMBL80 (Naloxone, NSC-70413, Nalone, Narcanti, Narcan, 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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  • 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]
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]-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]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]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 [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 DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.84 pIC50 1461 nM IC50 DrugMatrix in vitro pharmacology data
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 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 cell membranes B 6.86 pIC50 138 nM IC50 J. Nat. Prod. (2007) 70: 872-875 [PMID:17451272]
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 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]
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]
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 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
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 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 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 B 8.04 pKi 9.2 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2006-2012 [PMID:18313920]
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 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]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 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]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 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 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 at from guinea pig cortical tissue B 7.18 pKi 66 nM Ki J. Med. Chem. (1993) 36: 2833-2841 [PMID:8410998]
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 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]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]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-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]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]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-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-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 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 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 B 8.43 pKi 3.7 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2006-2012 [PMID:18313920]
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 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 after 150 mins by liquid scintillation counting method B 8.64 pKi 2.3 nM Ki MedChemComm (2016) 7: 317-326
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 [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 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 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 B 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 B 7.35 pIC50 45 nM IC50 J Med Chem (2017) 60: 6733-6750 [PMID:28726402]
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 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 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 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 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]
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