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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) |
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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 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]