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Meperidine (CID 4058) - Compound BioActivity Data
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BioActivity Outcomes:
Active(13)
 
 
Inactive(1)
 
 
Inconclusive(7)
 
 
Unspecified(76)
 
 
Top Targets:
7TM GPCR Srx(8)
 
 
 
p450(7)
 
 
 
7TM GPCR Srsx(4)
 
 
ERG2 Sigma1R(3)
 
 
SLC6sbd SERT(2)
 
 
 
BioAssay Types:
Literature(94)
 
 
 
 
 
BioActivity Types:
IC50(9)
 
 
 
Ki(4)
 
 
 
EC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 87    Data Row: 97   Total Pages: 5   Display: Page     
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#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]
pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005 [AID781328, Type: Literature]
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