Oxymorphone (CID 5284604) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(32)
 
 
Inactive(2)
 
 
Inconclusive(7)
 
 
Unspecified(20)
 
 
Top Targets:
7TM GPCR Srx(4)
 
 
 
GT1 Gtf like(2)
 
 
BioAssay Types:
Literature(57)
 
 
 
 
BioActivity Types:
Ki(20)
 
 
IC50(8)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 61    Data Row: 61   Total Pages: 2   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103250876]
IC50 1.3e-05Concentration for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the absence of NaCl [AID149036, Type: Literature]
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2
[SID103250876]
IC50 0.00015Concentration for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the presence of NaCl [AID149037, Type: Literature]
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3
[SID103250876]
Ki 0.00054Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting [AID603730, Type: Literature]Mu-type opioid receptor [gi:3024265]
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4
[SID103250876]
Ki 0.00078Inhibitory 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) [AID148058, Type: Literature]
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5
[SID103250876]
Ki 0.00097Inhibition of [3H]DAMGO binding to opioid receptor mu from rat brain membranes [AID239182, Type: Literature]
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6
[SID103250876]
IC50 0.0014Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane [AID148993, Type: Literature]
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7
[SID103250876]
Ki 0.015Binding affinity against Opioid receptor mu 1 of guinea pig brain membranes using 0.5 nM of [3H]naloxone as radioligand [AID148045, Type: Literature]Mu-type opioid receptor [gi:3024265]
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8
[SID103250876]
Ki 0.0174Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells [AID152389, Type: Literature]
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9
[SID103250876]
Ki 0.0231Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 [AID152387, Type: Literature]
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10
[SID103250876]
ED50 0.024Analgesic potency (antinociceptive activity) (administered icv) at peak time of 10 min in male Swiss-Webster mice [AID128651, Type: Literature]
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11
[SID103250876]
IC50 0.024Agonist activity in the guinea pig ileum longitudinal muscle myenteric plexus. [AID78000, Type: Literature]
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12
[SID103250876]
Ki 0.0262Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 [AID152385, Type: Literature]
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13
[SID103250876]
Ki 0.0427Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain homogenate by scintillation counting [AID603729, Type: Literature]
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14
[SID103250876]
IC50 0.045Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane [AID149630, Type: Literature]
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15
[SID103250876]
Ki 0.05Inhibitory 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) [AID150036, Type: Literature]
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16
[SID103250876]
Ki 0.0576Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting [AID603728, Type: Literature]Kappa-type opioid receptor [gi:730228]
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17
[SID103250876]
Ki 0.0616Inhibition of [3H]U-69593 binding to opioid receptor kappa from guinea pig brain membranes [AID239358, Type: Literature]
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18
[SID103250876]
IC50 0.077Agonist activity in the mouse vas deferens. [AID132333, Type: Literature]
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19
[SID103250876]
Ki 0.0805Inhibition of [3H][Ile5,6]deltorphin II binding to opioid receptor delta from rat brain membranes [AID239441, Type: Literature]
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20
[SID103250876]
IC50 0.09Inhibition of total opioid receptor by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane [AID148475, Type: Literature]
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21
[SID103250876]
Ki 0.095Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells [AID148584, Type: other]
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22
[SID103250876]
Ki 0.137Inhibitory 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). [AID149439, Type: Literature]
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23
[SID103250876]
Ki 0.145Binding affinity against Opioid receptor delta 1 of guinea pig brain membranes using 1 nM of [3H]DADLE as radioligand [AID149913, Type: Literature]
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24
[SID103250876]
Ki 0.208Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells [AID148586, Type: Literature]
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25
[SID103250876]
Ki 0.435Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells [AID148585, Type: Literature]
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26
[SID103250876]
Ki 0.61Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells [AID149086, Type: Literature]
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27
[SID103250876]
IC50 0.63Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane [AID147960, Type: Literature]
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28
[SID103250876]
Ki 0.725Binding affinity against Opioid receptor kappa 1 of guinea pig brain membranes using 1 nM of (-)-[3H]ethylketazocine as radioligand [AID149409, Type: Literature]Kappa-type opioid receptor [gi:730228]
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29
[SID103250876]
Ki 0.73Displacement of [3H]- diprenorphine from delta-receptor expressed in HEK 293 cells [AID149087, Type: Literature]
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30
[SID103250876]
 Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604020, Type: Literature]
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31
[SID103250876]
 Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678721, Type: Literature]
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32
[SID48416368]
 DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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33
[SID103250876]
 Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain homogenate to Ki for kappa opioid receptor in guinea pig cerebellum homogenate [AID603731, Type: Literature]
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34
[SID103250876]
 Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset [AID588220, Type: Literature]
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35
[SID103250876]
 Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain homogenate to Ki for kappa opioid receptor in guinea pig cerebellum homogenate [AID603727, Type: Literature]
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36
[SID103250876]
 Specific activity of expressed human recombinant UGT2B7H [AID624620, Type: Literature]UDP-glucuronosyltransferase 2B7 [gi:136727]
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37
[SID103250876]
 Specific activity of expressed human recombinant UGT2B7Y [AID624621, Type: Literature]UDP-glucuronosyltransferase 2B7 [gi:136727]
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38
[SID103250876]
 Ratio of binding affinities for opioid receptors delta and mu [AID244113, Type: Literature]Mu-type opioid receptor [gi:464314]
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39
[SID103250876]
 Ratio of binding affinities for opioid receptors kappa and mu [AID244114, Type: Literature]Mu-type opioid receptor [gi:464314]
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40
[SID103250876]
 Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604021, Type: Literature]
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41
[SID103250876]
 Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604022, Type: Literature]
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42
[SID103250876]
 Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604023, Type: Literature]
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43
[SID103250876]
 Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr [AID604024, Type: Literature]
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44
[SID103250876]
 Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604025, Type: Literature]
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45
[SID103250876]
 Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents [AID588213, Type: Literature]
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46
[SID103250876]
 Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents [AID588212, Type: Literature]
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47
[SID103250876]
 Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans [AID588211, Type: Literature]
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48
[SID103250876]
 The ability of compound was measured to replace [3H]-labeled [D-Ala2, Met5]-enkephalinamide in rat brain homogenates by using [3H]-opiate binding assay [AID195694, Type: Literature]
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49
[SID103250876]
 Ratio for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the absence of NaCl to that of presence of NaCl [AID231774, Type: Literature]
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50
[SID103250876]
 Percent analgesia of compound was measured in mice by using tail-flick assay [AID111971, Type: Literature]
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