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BioActivity Data for Compound Naloxone (CID 5284596)

BioActivity Outcomes:
Active(186)
 
 
Inactive(135)
 
 
Inconclusive(28)
 
 
Unspecified(570)
 
 
Top Targets:
7tm 4(175)
 
 
 
 
 
ERG2 Sigma1R(14)
 
 
 
 
p450(10)
 
 
 
 
GT1 Gtf like(10)
 
 
NR LBD ER(9)
 
 
 
BioAssay Types:
Literature(469)
 
 
 
 
 
Confirmatory(189)
 
 
 
 
 
Summary(24)
 
 
 
Screening(20)
 
 
BioAssay Categories:
In vitro(10)
 
 
 
In vivo(21)
 
 
 
 
Biochemical(121)
 
 
 
 
 
Toxicity(6)
 
 
ADME(45)
 
 
Cell-based(23)
 
 
 
 
BioActivity Types:
IC50(182)
 
 
 
 
 
Potency(86)
 
 
 
Ki(75)
 
 
 
 
Kd(26)
 
 
EC50(10)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 884    Data Row: 919   Total Pages: 46   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 0.00068Affinity 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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11
[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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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 0.001Displacement of [3H]-(-)-naloxone from opiate receptor in rat brain membrane [AID1135637, Type: Literature]Sigma non-opioid intracellular receptor 1 [gi:81882051]
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15
[SID103170037]
Kd 0.001Displacement of [3H]-(-)-naloxone from opiate receptor in rat brain membrane [AID1135637, Type: Literature]Mu-type opioid receptor [gi:464314]
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16
[SID103170037]
Kd 0.001Displacement of [3H]-(-)-naloxone from opiate receptor in rat brain membrane [AID1135637, Type: Literature]Delta-type opioid receptor [gi:464311]
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17
[SID103170037]
Kd 0.001Displacement of [3H]-(-)-naloxone from opiate receptor in rat brain membrane [AID1135637, Type: Literature]Kappa-type opioid receptor [gi:464313]
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18
[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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19
[SID103170037]
Ki 0.00107Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. [AID151900, Type: Literature]
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20
[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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