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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) |
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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 32:
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]