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Naloxone (CID 5284596) - Compound BioActivity Data
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BioActivity Outcomes:
Active(167)
 
 
Inactive(132)
 
 
Inconclusive(28)
 
 
Unspecified(551)
 
 
Top Targets:
7TM GPCR Srx(124)
 
 
 
 
 
7TM GPCR Srsx(43)
 
 
 
 
 
ERG2 Sigma1R(12)
 
 
 
 
GT1 Gtf like(10)
 
 
p450(10)
 
 
 
 
BioAssay Types:
Literature(432)
 
 
 
 
 
Confirmatory(186)
 
 
 
 
 
Summary(24)
 
 
 
Screening(20)
 
 
BioActivity Types:
IC50(179)
 
 
 
 
 
Potency(86)
 
 
 
Ki(74)
 
 
 
 
Kd(22)
 
 
EC50(6)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 849    Data Row: 878   Total Pages: 44   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 response 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 0.0011Displacement 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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17
[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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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]
IC50 0.0014Inhibition of [3H]-Naloxone binding to rat brain membrane without NaCl [AID226060, Type: Literature]
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