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Naloxone (CID 5284596) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(165)
 
 
Inactive(129)
 
 
Inconclusive(28)
 
 
Unspecified(354)
 
 
Top Targets:
7TM GPCR Srx(119)
 
 
 
 
 
7TM GPCR Srsx(42)
 
 
 
 
 
ERG2 Sigma1R(12)
 
 
 
 
p450(10)
 
 
 
 
GT1 Gtf like(10)
 
 
BioAssay Types:
Literature(422)
 
 
 
 
 
Confirmatory(69)
 
 
 
Summary(24)
 
 
 
Screening(20)
 
 
BioActivity Types:
IC50(178)
 
 
 
 
 
Potency(85)
 
 
 
Ki(74)
 
 
 
 
Kd(22)
 
 
EC50(6)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 647    Data Row: 676   Total Pages: 14   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103170037]
IC50 4e-06Concentration 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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2
[SID103170037]
IC50 9e-06Concentration 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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3
[SID103170037]
Kd 0.000219Antagonist activity against mu opioid receptor assessed as effect on endomorphin-2-induced calcium reponse in CHO cells by aequorin luminescence based calcium assay [AID277679, Type: Literature]Mu-type opioid receptor [gi:2851402]
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4
[SID103170037]
Ki 0.00023Displacement of [3H]DAMGO from human mu-opioid receptor expressed in CHO cells after 60 mins by scintillation counting [AID596551, Type: Literature]Mu-type opioid receptor [gi:2851402]
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5
[SID103170037]
Ki 0.00025Displacement of [3H]U69563 from human kappa-opioid receptor expressed in CHO cells after 60 mins by scintillation counting [AID596552, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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6
[SID103170037]
Kd 0.0004Opioid receptor mu 1 affinity against the receptor site model site 1 (mu1) [AID151464, Type: Literature]Mu-type opioid receptor [gi:464314]
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7
[SID103170037]
Ki 0.000562Displacement of [3H]DPN from human recombinant mu-type opioid receptor expressed in CHO cell membranes [AID600431, Type: Literature]Mu-type opioid receptor [gi:2851402]
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8
[SID103170037]
Ki 0.00057Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells [AID603171, Type: Literature]
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9
[SID103170037]
Ki 0.00066Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells [AID410718, Type: Literature]Mu-type opioid receptor [gi:2851402]
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10
[SID103170037]
Ki 0.00068Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membrane [AID295932, Type: Literature]Mu-type opioid receptor [gi:3024265]
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11
[SID103170037]
Ki 0.00068Affinity to mu-receptor, using [3H]DAMGO as radioligand in homogenates of guinea pig brain membranes [AID152225, Type: Literature]Mu-type opioid receptor [gi:3024265]
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12
[SID103170037]
Ki 0.00079Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells [AID286302, Type: Literature]Mu-type opioid receptor [gi:2851402]
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13
[SID103170037]
Ki 0.00098Displacement of [125I]OXY from human mu opioid receptor expressed in CHO cells [AID443797, Type: Literature]Mu-type opioid receptor [gi:2851402]
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14
[SID103170037]
Kd 0.001Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa) [AID148456, Type: Literature]
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15
[SID103170037]
Ki 0.00107Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. [AID151900, Type: Literature]
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16
[SID103170037]
Ki 0.0011In vivo binding affinity against mu opioid receptor was measured by using labeled ligand [3H]naloxone (0.5 nM) [AID141512, Type: Literature]Mu-type opioid receptor [gi:3024265]
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17
[SID103170037]
Ki 0.0011Displacement of [3H]U-69593 from human opioid kappa receptor expressed in CHO cells [AID286303, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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18
[SID103170037]
Ki 0.0012Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 expressed in HEK 293 cells [AID148018, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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19
[SID103170037]
Ki 0.0012Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells [AID410720, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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20
[SID103170037]
Ki 0.0014Inhibition of [3H]DAMGO binding to rat Opioid receptor mu 1 [AID151759, Type: Literature]Mu-type opioid receptor [gi:464314]
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21
[SID103170037]
IC50 0.0014Inhibition of [3H]-Naloxone binding to rat brain membrane without NaCl [AID226060, Type: Literature]
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22
[SID103170037]
IC50 0.0015Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand [AID147859, Type: Literature]
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23
[SID103170037]
Ki 0.0015Binding affinity to mu opioid receptor [AID437485, Type: Literature]
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24
[SID103170037]
Ki 0.0016Displacement of [3H]DAGO from mu opioid receptor [AID338153, Type: Literature]
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25
[SID103170037]
IC50 0.0016Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA [AID255079, Type: Literature]Adenosine receptor A3 [gi:1351831]
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26
[SID103170037]
Kd 0.00186Negative logarithm of the molar concentration of Opioid receptor mu 1 was determined in guinea pig ileum [AID148202, Type: Literature]Mu-type opioid receptor [gi:3024265]
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27
[SID103170037]
IC50 0.002Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl [AID150392, Type: Literature]
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28
[SID103170037]
IC50 0.002Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl [AID149041, Type: Literature]
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29
[SID103170037]
IC50 0.002Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand [AID152239, Type: Literature]
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30
[SID103170037]
Ki 0.00227Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells [AID603170, Type: Literature]
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31
[SID103170037]
Ki 0.0026Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum by beta plate scintillation counting [AID487869, Type: Literature]
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32
[SID103170037]
Kd 0.00295Narcotic antagonistic potency evaluated in morphine-induced Straub tail phenomenon in mice [AID123368, Type: Literature]
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33
[SID103170037]
Kd 0.003Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor mu 1 [AID151585, Type: Literature]
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34
[SID103170037]
Ki 0.003Displacement of [125I]OXY from human kappa opioid receptor expressed in CHO cells [AID443796, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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35
[SID103170037]
Kd 0.00316Tested for its antagonist activity against mu receptor using DAMGO as radioligand in isolated guinea pig ileum [AID224714, Type: Literature]Mu-type opioid receptor [gi:3024265]
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36
[SID103170037]
Ki 0.00317Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane [AID295930, Type: Literature]Kappa-type opioid receptor [gi:730228]
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37
[SID103170037]
Ki 0.0032Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes [AID148988, Type: Literature]Kappa-type opioid receptor [gi:730228]
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38
[SID103170037]
Ki 0.00363In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement. [AID150975, Type: Literature]
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39
[SID103170037]
Ki 0.0037Inhibition of binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human mu opioid receptor [AID150990, Type: Literature]
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40
[SID103170037]
Ki 0.0037Binding affinity towards mu opioid receptor by displacement of [3H]NAL from rat brain homogenates [AID224718, Type: Literature]
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41
[SID103170037]
Ki 0.0037Tested for binding affinity towards mu receptor in presence of [3H]NAL radioligand [AID141762, Type: Literature]
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42
[SID103170037]
Ki 0.0037Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells [AID274390, Type: Literature]Mu-type opioid receptor [gi:2851402]
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43
[SID103170037]
Ki 0.0037Displacement of [3H]diprenorphine from human cloned mu opioid receptor [AID325957, Type: Literature]Mu-type opioid receptor [gi:2851402]
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44
[SID103170037]
Ki 0.0037Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells [AID274411, Type: Literature]Mu-type opioid receptor [gi:2851402]
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45
[SID103170037]
Ki 0.0039Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain by beta plate scintillation counting [AID487867, Type: Literature]
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46
[SID103170037]
Ki 0.00423Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells [AID603169, Type: Literature]
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47
[SID103170037]
Ki 0.00447Displacement of [3H]DPN from human recombinant kappa-type opioid receptor expressed in CHO cell membranes [AID600433, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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48
[SID103170037]
Kd 0.0045Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor kappa 1 [AID148459, Type: Literature]
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49
[SID103170037]
IC50 0.005Inhibition of 0.5 nM [3H]- Bremazocine binding to Opioid receptor mu 1 of bovine striatum membrane [AID149445, Type: Literature]Mu-type opioid receptor [gi:6093615]
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50
[SID103170037]
Kd 0.005Opioid receptor mu 2 affinity against the receptor site model site 2(mu2) [AID152211, Type: Literature]Mu-type opioid receptor [gi:464314]
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