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Meperidine (CID 4058) - Compound BioActivity Data
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BioActivity Outcomes:
Active(13)
 
 
Inactive(1)
 
 
Inconclusive(7)
 
 
Unspecified(75)
 
 
Top Targets:
7TM GPCR Srx(8)
 
 
 
p450(7)
 
 
 
7TM GPCR Srsx(4)
 
 
ERG2 Sigma1R(3)
 
 
SLC6sbd SERT(2)
 
 
 
BioAssay Types:
Literature(91)
 
 
 
 
 
BioActivity Types:
IC50(9)
 
 
 
Ki(4)
 
 
 
EC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 86    Data Row: 96   Total Pages: 2   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103184537]
IC50 0.315Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand [AID152239, Type: Literature]
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2
[SID103184537]
IC50 0.32359Inhibitory concentration against potassium channel HERG [AID243151, Type: Literature]
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3
[SID103184537]
Ki 0.412Displacement of [3H]paroxetine from serotonin transporter (SERT) [AID204538, Type: Literature]Sodium-dependent serotonin transporter [gi:400629]
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4
[SID103184537]
Ki 0.451Binding affinity against mu opioid receptor was determined in brain membrane preparations from male Hartley guinea-pigs [AID141504, Type: Literature]Mu-type opioid receptor [gi:3024265]
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5
[SID103184537]
IC50 0.5Tested for displacement of radioligand [3H]-Naloxone from opiate receptor [AID145928, Type: Literature]
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6
[SID103184537]
IC50 0.5Inhibition of Opioid receptors with [3H]naloxone binding in the absence of NaCl [AID150234, Type: Literature]
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7
[SID103184537]
IC50 2.37Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand [AID147859, Type: Literature]
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8
[SID103184537]
EC50 9.4Agonist activity at human cloned mu opioid receptor by [35S]GTPgammaS binding assay [AID392933, Type: Literature]Mu-type opioid receptor [gi:2851402]
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9
[SID103184537]
Ki 17.8Displacement of [3H]WIN-35428 from dopamine transporter (DAT) [AID65195, Type: Literature]Sodium-dependent dopamine transporter [gi:128613]
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10
[SID103184537]
IC50 40Inhibition of Opioid receptors binding by inhibiting specific [3H]naloxone binding by 50% in the presence of 100 mM NaCl [AID150235, Type: Literature]
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11
[SID103184537]
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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12
[SID48416212]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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13
[SID85209612]
Ligands of peptide (Class A) GPCRs [AID2063, Type: other]
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14
[SID103184537]
IC50 10Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand [AID148078, Type: Literature]
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15
[SID103184537]
IC50 74.131Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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16
[SID103184537]
IC50 75.8578Inhibition of human ERG channel in HEK293 cells by voltage-clamp method [AID392051, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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17
[SID103184537]
Ki 100Binding affinity against Opioid receptor kappa 1 was determined in brain membrane preparations from male Hartley guinea-pigs [AID149142, Type: Literature]Kappa-type opioid receptor [gi:730228]
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18
[SID103184537]
Km 1900Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay [AID456232, Type: Literature]Liver carboxylesterase 1 [gi:119576]
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19
[SID103184537]
Relative affinity for dopamine and serotonin transporters [AID235172, Type: Literature]Sodium-dependent dopamine transporter [gi:128613]
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20
[SID103184537]
Specific activity of expressed human recombinant UGT1A4 [AID624608, Type: Literature]UDP-glucuronosyltransferase 1-4 [gi:136731]
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21
[SID103184537]
Clinically relevant substrates of human liver microsomal P450 enzymes, isoform CYP2B6 [AID589033, Type: other]Cytochrome P450 2B6 [gi:117205]
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22
[SID103184537]
Intrinsic activity at human cloned mu opioid receptor at 100 uM by [35S]GTPgammaS binding assay relative to DAMGO [AID392934, Type: Literature]Mu-type opioid receptor [gi:2851402]
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23
[SID103184537]
The ratio between [3H]naloxone binding in the presence and absence of 100 mM NaCl [AID149046, Type: Literature]Sigma non-opioid intracellular receptor 1 [gi:81882051]
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24
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the presence of 100 mM NaCl [AID149035, Type: Literature]Sigma non-opioid intracellular receptor 1 [gi:81882051]
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25
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the absence of NaCl [AID149034, Type: Literature]Sigma non-opioid intracellular receptor 1 [gi:81882051]
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26
[SID103184537]
Effective dose to show narcotic analgesic activity was evaluated in mouse tail-flick test when administered subcutaneously [AID131898, Type: Literature]
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27
[SID103184537]
Relative Analgesic activity of compound to the N-methyl homologue assayed by the mouse hotplate method [AID136959, Type: Literature]
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28
[SID103184537]
Ratio of IC50 values for incubations in the presence of 100 mM NaCl to those incubations in its absence [AID150236, Type: Literature]
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29
[SID103184537]
Relative affinity for dopamine and serotonin transporters [AID235172, Type: Literature]Sodium-dependent serotonin transporter [gi:400629]
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30
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the absence of NaCl [AID149034, Type: Literature]Delta-type opioid receptor [gi:464311]
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31
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the presence of 100 mM NaCl [AID149035, Type: Literature]Delta-type opioid receptor [gi:464311]
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32
[SID103184537]
The ratio between [3H]naloxone binding in the presence and absence of 100 mM NaCl [AID149046, Type: Literature]Delta-type opioid receptor [gi:464311]
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33
[SID103184537]
The ratio between [3H]naloxone binding in the presence and absence of 100 mM NaCl [AID149046, Type: Literature]Kappa-type opioid receptor [gi:464313]
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34
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the presence of 100 mM NaCl [AID149035, Type: Literature]Kappa-type opioid receptor [gi:464313]
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35
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the absence of NaCl [AID149034, Type: Literature]Kappa-type opioid receptor [gi:464313]
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36
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the absence of NaCl [AID149034, Type: Literature]Mu-type opioid receptor [gi:464314]
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37
[SID103184537]
Inhibition of [3H]naloxone receptor binding to opioid receptor in the presence of 100 mM NaCl [AID149035, Type: Literature]Mu-type opioid receptor [gi:464314]
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38
[SID103184537]
The ratio between [3H]naloxone binding in the presence and absence of 100 mM NaCl [AID149046, Type: Literature]Mu-type opioid receptor [gi:464314]
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39
[SID103184537]
Unbound fraction (plasma) [AID7783, Type: Literature]
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40
[SID103184537]
Observed volume of distribution [AID8002, Type: Literature]
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41
[SID103184537]
Ionization constant (pKa) [AID26362, Type: Literature]
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42
[SID103184537]
Delta logD (logD6.5 - logD7.4) [AID27167, Type: Literature]
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43
[SID103184537]
Partition coefficient (logD6.5) [AID28681, Type: other]
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44
[SID103184537]
Ionization constant (pKa) [AID29359, Type: other]
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45
[SID103184537]
Oral bioavailability in human [AID29813, Type: Literature]
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46
[SID103184537]
Effective dose for antinociceptive activity in mice hot plate test s.c. [AID114683, Type: Literature]
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47
[SID103184537]
Effective dose required for analgesic potency in the hotplate procedure after sc injection into mice. [AID114834, Type: Literature]
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48
[SID103184537]
Permeability coefficient in human skin [AID311367, Type: Literature]
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49
[SID103184537]
Analgesic activity in albino mouse assessed as response latency time to pain stimulus at 5 mg/kg, ip after 1 hr by hot plate method [AID416491, Type: Literature]
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50
[SID103184537]
Analgesic activity in albino mouse assessed as response latency time to pain stimulus at 5 mg/kg, ip after 3 hrs by hot plate method [AID416493, Type: Literature]
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