oxymorphone [Ligand Id: 7094] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL963 (14-hydroxydihydromorphinone, 7,8-dihydro-14-hydroxymorphinone, Dihydroxymorphinone, IDS-NO-003, NIH 10323, NSC-19045, Numorphan, Opana, Oxycodone hydrochloride impurity, oxymorphone-, Oxymorphone, Oxymorphone cii)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Binding affinity against Opioid receptor delta 1 of guinea pig brain membranes using 1 nM of [3H]DADLE as radioligand B 6.84 pKi 145 nM Ki J Med Chem (1986) 29: 1222-1225 [PMID:2879914]
ChEMBL Displacement of [3H]-diprenorphine from recombinant human DOR expressed in CHO cell membranes after 60 mins by liquid scintillation counting B 7.15 pKi 70 nM Ki J Med Chem (2017) 60: 9407-9412 [PMID:29053268]
ChEMBL Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor delta 1 at a a temperature 25 degree Celsius labeled with [3H](D-Ala2-D-Leu5)-enkephalin (0.7 nM) B 7.3 pKi 50 nM Ki J Med Chem (1985) 28: 974-976 [PMID:2409281]
ChEMBL Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane B 7.35 pIC50 45 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 Displacement of [3H]- diprenorphine from delta-receptor expressed in HEK 293 cells B 6.14 pKi 730 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]-DPDPE from mouse DOR expressed in HEK293 cells B 6.14 pKi 724.44 nM Ki ACS Med Chem Lett (2012) 3: 640-644 [PMID:23585918]
ChEMBL Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells B 6.21 pKi 610 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Inhibition of [3H][Ile5,6]deltorphin II binding to opioid receptor delta from rat brain membranes B 7.09 pKi 80.5 nM Ki J Med Chem (2005) 48: 3372-3378 [PMID:15857143]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]-HS665 from recombinant human KOR expressed in CHO cell membranes after 30 mins by liquid scintillation counting B 7.6 pKi 25.3 nM Ki J Med Chem (2017) 60: 9407-9412 [PMID:29053268]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells B 6.36 pKi 435 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells B 6.68 pKi 208 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells B 7.02 pKi 95 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity against Opioid receptor kappa 1 of guinea pig brain membranes using 1 nM of (-)-[3H]ethylketazocine as radioligand B 6.14 pKi 725 nM Ki J Med Chem (1986) 29: 1222-1225 [PMID:2879914]
ChEMBL Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor kappa 1 at temperature 25 degree Celsius labeled with (-)-[3H]immazocine (0.1 nM). B 6.86 pKi 137 nM Ki J Med Chem (1985) 28: 974-976 [PMID:2409281]
ChEMBL Inhibition of [3H]U-69593 binding to opioid receptor kappa from guinea pig brain membranes B 7.21 pKi 61.6 nM Ki J Med Chem (2005) 48: 3372-3378 [PMID:15857143]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting B 7.24 pKi 57.6 nM Ki Bioorg Med Chem Lett (2011) 21: 4104-4107 [PMID:21641798]
ChEMBL Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane B 6.2 pIC50 630 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]-DAMGO from recombinant human MOR expressed in CHO cell membranes after 60 mins by liquid scintillation counting B 8.75 pKi 1.79 nM Ki J Med Chem (2017) 60: 9407-9412 [PMID:29053268]
ChEMBL Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay F 8.11 pEC50 7.8 nM EC50 J Med Chem (2017) 60: 9407-9412 [PMID:29053268]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Displacement of [3H]-DAMGO from mouse MOR expressed in HEK293 cells B 8.3 pKi 5.01 nM Ki ACS Med Chem Lett (2012) 3: 640-644 [PMID:23585918]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 B 7.58 pKi 26.2 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 B 7.64 pKi 23.1 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells B 7.76 pKi 17.4 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Inhibition of [3H]DAMGO binding to opioid receptor mu from rat brain membranes B 9.01 pKi 0.97 nM Ki J Med Chem (2005) 48: 3372-3378 [PMID:15857143]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Binding affinity against Opioid receptor mu 1 of guinea pig brain membranes using 0.5 nM of [3H]naloxone as radioligand B 7.82 pKi 15 nM Ki J Med Chem (1986) 29: 1222-1225 [PMID:2879914]
ChEMBL Inhibitory binding constant in guinea pig brain homogenate was reported at mu site at a temperature 25 degree Centigrade labeled with [3H](D-Ala2-MePhe4,Gly-ol5)enkephalin(1 nM) B 9.11 pKi 0.78 nM Ki J Med Chem (1985) 28: 974-976 [PMID:2409281]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting B 9.27 pKi 0.54 nM Ki Bioorg Med Chem Lett (2011) 21: 4104-4107 [PMID:21641798]
ChEMBL Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane B 8.85 pIC50 1.4 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]

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]