oxycodone [Ligand Id: 7093] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL656 ((-)-14-hydroxydihydrocodeinone, 14-hydroxydihydrocodeinone, Dihydrone, IDS-NO-002, N02AA05, NSC-19043, Oxicone, Oxycodone, Oxycodone cii, Oxycontin, Oxymorphone 3-methyl ether, Pavinal, PF-00345439, Proladone, Pti 821, PTI-821, Remoxy, Xtampza, Xtampza er) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of electric eel AChE by Ellman's method | B | 4.12 | pIC50 | 76200 | nM | IC50 | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| ChEMBL | Displacement of [3H[Ile5,6]-deltorphin II from delta opioid receptor of rat brain membranes | B | 5.96 | pKi | 1087 | nM | Ki | J Med Chem (2005) 48: 5052-5055 [PMID:16033285] |
| ChEMBL | Displacement of [3H]Ile5,6-deltorphin-2 from DOR in Wistar rat brain membranes after 60 mins by liquid scintillation analysis | B | 6.31 | pKi | 487 | nM | Ki | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole cell patch clamp assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 15508-15526 [PMID:33064947] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 4.8 | pEC50 | 16000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 4.8 | pEC50 | 16000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor of rat brain membranes | B | 5.58 | pKi | 2658 | nM | Ki | J Med Chem (2005) 48: 5052-5055 [PMID:16033285] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| ChEMBL | Displacement of [3H]HS-665 from KOR in guinea pig brain membranes after 60 mins by liquid scintillation analysis | B | 6.49 | pKi | 325 | nM | Ki | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Scintillation Proximity Assay (SPA): Briefly, serial dilutions of the test compounds were placed in a 96-well plate to which were added SPA beads, membrane and radioligand. The assay conditions for each opioid receptor subtype are described in Table 10 below. The plates were incubated for 8 hours-overnight at room temperature, spun at 1000 rpm to pellet the SPA beads, and radioactivity was measured using the TopCount microplate Scintillation counter. Specific binding at each concentration of test compound was calculated by subtracting the non-specific binding measured in the presence of excess cold ligand. IC50 values were obtained by non-linear regression of specific binding versus concentration curves and Ki values were calculated using Kd values that were experimentally pre-determined for each lot of membrane preparations. | B | 6.87 | pKi | 133.48 | nM | Ki | US-9233167-B2. Oligomer-opioid agonist conjugates (2016) |
| ChEMBL | Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2020) 63: 2434-2454 [PMID:31743642] |
| ChEMBL | Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2020) 63: 15508-15526 [PMID:33064947] |
| ChEMBL | Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 60 mins measured by MicroBeta scintillation counter method | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2021) 64: 10139-10154 [PMID:34236190] |
| ChEMBL | Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.3 | pEC50 | 500 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| ChEMBL | HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response. | F | 6.32 | pEC50 | 478 | nM | EC50 | US-9233167-B2. Oligomer-opioid agonist conjugates (2016) |
| ChEMBL | Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay | F | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2020) 63: 2434-2454 [PMID:31743642] |
| ChEMBL | Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay | F | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2020) 63: 15508-15526 [PMID:33064947] |
| ChEMBL | Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay | F | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2021) 64: 10139-10154 [PMID:34236190] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.8 | pEC50 | 160 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor of rat brain membranes | B | 7.36 | pKi | 43.6 | nM | Ki | J Med Chem (2005) 48: 5052-5055 [PMID:16033285] |
| ChEMBL | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes after 60 mins by liquid scintillation analysis | B | 8.05 | pKi | 8.9 | nM | Ki | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
| ChEMBL | Agonist activity at MOR in Wistar rat brain membranes after 60 mins by [35S]-GTPgammaS binding assay | F | 7.6 | pEC50 | 25 | nM | EC50 | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor expressed in HEK293 membranes incubated for 120 mins by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2020) 63: 2434-2454 [PMID:31743642] |
| ChEMBL | Displacement of 3H](+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2020) 63: 15508-15526 [PMID:33064947] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor transfected in HEK293 membranes incubated for 120 mins measured by microBeta scintillation counter method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 10139-10154 [PMID:34236190] |
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]
