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, Oximorfona, 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 35:

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]