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norbinaltorphimine (CID 5480230) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(223)
 
 
Inactive(106)
 
 
Inconclusive(11)
 
 
Unspecified(131)
 
 
Top Targets:
7TM GPCR Srx(83)
 
 
 
 
7TM GPCR Srsx(34)
 
 
 
 
PIKKc TOR(4)
 
 
Pyr redox dim(4)
 
 
PLDc mTdp1 2(3)
 
 
BioAssay Types:
Literature(370)
 
 
 
 
Confirmatory(101)
 
 
 
 
BioActivity Types:
Ki(108)
 
 
Potency(99)
 
 
 
 
IC50(17)
 
 
EC50(6)
 
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 449    Data Row: 471   Total Pages: 10   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103698780]
Ki 2.7e-05Displacement 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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2
[SID103698780]
Ki 3.8e-05Functional antagonism was obtained by the ability of compound to inhibit stimulation of [35S]GTP gamma S binding produced by selective agonists U69,593 in guinea pig caudate membranes [AID77794, Type: Literature]
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3
[SID103698780]
Ki 3.8e-05Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor kappa 1 in Guinea pig Caudate stimulated by U69,593 [AID149428, Type: Literature]Kappa-type opioid receptor [gi:730228]
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4
[SID103698780]
Ki 3.8e-05Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (U69593, kappa-receptor), in guinea pig caudate membranes [AID149437, Type: Literature]Kappa-type opioid receptor [gi:730228]
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5
[SID103698780]
Ki 3.9e-05Compound was evaluated for its binding affinity by displacing [3H]U-69593 to human cloned Kappa opioid receptor transfected into CHO cells using [35S]GTP-gamma-S, assay [AID148016, Type: Literature]
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6
[SID103698780]
Ki 7e-05Antagonist activity on agonist (U50,488) stimulated [35S]GTP-gamma-S, binding in cloned opioid receptor kappa 1 [AID147989, Type: Literature]
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7
[SID103698780]
Ki 7e-05Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells [AID148587, Type: Literature]
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8
[SID103698780]
Ki 0.00012Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. [AID148588, Type: Literature]
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9
[SID103698780]
Ki 0.00012Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM U69,593 as the agonist ligand for kappa-receptor) [AID148990, Type: Literature]Kappa-type opioid receptor [gi:730228]
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10
[SID103698780]
Ki 0.00013Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor kappa 1 in COS-7 cells [AID148177, Type: Literature]
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11
[SID103698780]
Ki 0.000153Displacement of [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting [AID631359, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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12
[SID103698780]
Ki 0.00019Displacement of [125I]-IBNalA from KOR-1 expressed in CHO cells [AID603175, Type: Literature]
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13
[SID103698780]
Ki 0.0002Binding affinity against cloned human Opioid receptor kappa 1 transfected into chinese hamster ovary cells using [3H]U-69593 as radioligand [AID148013, Type: Literature]
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14
[SID103698780]
Ki 0.0002Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. [AID147987, Type: Literature]
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15
[SID103698780]
Ki 0.0002Ability to displace [3H]U-69593 from human recombinant Opioid receptor kappa 1 in CHO cells [AID147988, Type: Literature]
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16
[SID103698780]
Ki 0.0002Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor kappa 1 by displacing [3H]U-69593 [AID148017, Type: Literature]
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17
[SID103698780]
Ki 0.0002Binding affinity towards human cloned Opioid receptor kappa 1 using [3H]U-69593 [AID148007, Type: Literature]
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18
[SID103698780]
Ki 0.0002Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells [AID239386, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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19
[SID103698780]
Ki 0.00023Displacement of [125I]-IBNtxA from KOR-1 expressed in CHO cells [AID603174, Type: Literature]
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20
[SID103698780]
Ki 0.00024Displacement of [3H]diprenorphine from delta-W284E-receptor expressed in HEK 293 cells [AID148583, Type: Literature]
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21
[SID103698780]
Ki 0.00026Binding affinity of compound was measured against Opioid receptor kappa 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM preparation using U-50,488H as agonist [AID149136, Type: Literature]Kappa-type opioid receptor [gi:730228]
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22
[SID103698780]
Ki 0.00028Binding affinity for k opioid receptor was determined using [3H]U-69593 radioligand in Guinea pig brain membranes [AID149144, Type: Literature]Kappa-type opioid receptor [gi:730228]
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23
[SID103698780]
Ki 0.00028Binding affinity determined on Opioid receptor kappa 1 in Guinea pig brain membranes using radioligand [3H]U-69593 [AID149125, Type: Literature]Kappa-type opioid receptor [gi:730228]
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24
[SID103698780]
Ki 0.00028The binding affinity on kappa-opioid receptor using [3H]- U-69,593 as radioligand [AID149551, Type: Literature]Kappa-type opioid receptor [gi:730228]
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25
[SID103698780]
Ki 0.0003Antagonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of compound 14-induced [35S]GTPgammaS binding [AID450030, Type: Literature]
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26
[SID103698780]
Ki 0.00034Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells [AID481097, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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27
[SID103698780]
Ki 0.00036Binding affinity towards cloned human Opioid receptor kappa 1 in CHO cell membranes. [AID148010, Type: Literature]
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28
[SID103698780]
Ki 0.00037In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement. [AID148006, Type: Literature]
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29
[SID103698780]
Ki 0.00039Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells [AID152388, Type: Literature]
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30
[SID103698780]
Ki 0.0004Inhibition of [3H]diprenorphine binding to human opioid receptor kappa 1 expressed in CHO cells [AID239262, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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31
[SID103698780]
Ki 0.00077Mutant factor against mu-[K303E] with Opioid receptor kappa 1 for binding affinity [AID148597, Type: Literature]
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32
[SID103698780]
Ki 0.0008Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry [AID450017, Type: Literature]
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33
[SID103698780]
Ki 0.00081Binding affinity was measured on opioid receptor kappa 1 [AID149267, Type: Literature]Kappa-type opioid receptor [gi:730228]
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34
[SID103698780]
Ki 0.00085Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting [AID613641, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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35
[SID103698780]
Ki 0.000861Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum [AID574376, Type: Literature]Kappa-type opioid receptor [gi:730228]
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36
[SID103698780]
Ki 0.000861Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum [AID502177, Type: Literature]Kappa-type opioid receptor [gi:730228]
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37
[SID103698780]
Ki 0.0009Binding affinity to kappa opioid receptor [AID516471, Type: Literature]
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38
[SID103698780]
Ki 0.00094Binding affinity using [3H]diprenorphine as the radioligand against K303E Opioid receptor mu 1 in COS-7 cells [AID151123, Type: Literature]
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39
[SID103698780]
Ki 0.00109Binding affinity of compound for Opioid receptor kappa 1 was determined using [3H]U-69593 as radioligand from guinea pig caudate [AID149134, Type: Literature]Kappa-type opioid receptor [gi:730228]
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40
[SID103698780]
Ki 0.00109Ability to displace [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain [AID148981, Type: Literature]Kappa-type opioid receptor [gi:730228]
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41
[SID103698780]
Ki 0.00109Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain [AID149260, Type: Literature]Kappa-type opioid receptor [gi:730228]
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42
[SID103698780]
Ki 0.0012Inhibition of [3H]diprenorphine binding to rat Opioid receptor mu 1 expressed in C6 cells [AID239172, Type: Literature]
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43
[SID103698780]
Ki 0.00139Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells [AID148585, Type: Literature]
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44
[SID103698780]
Kd 0.00165Displacement of [3H]U69,593 from kappa opioid receptor in mouse brain tissue [AID381426, Type: Literature]Kappa-type opioid receptor [gi:464312]
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45
[SID103698780]
IC50 0.0021Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding [AID502618, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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46
[SID103698780]
IC50 0.0021Antagonist activity at human kappa opioid receptor assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding [AID516453, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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47
[SID103698780]
Ki 0.0027Displacement 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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48
[SID103698780]
IC50 0.00437Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488 [AID147854, Type: Literature]
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49
[SID103698780]
Ki 0.00442Compound was evaluated for functional opioid activity by stimulation of [35S]GTP-gamma-S, in cloned human Opioid receptor delta 1 transfected into CHO cells [AID148248, Type: Literature]
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50
[SID103698780]
IC50 0.0046Antagonist activity determined in the [35S]GTP-gamma-S, binding assay relative to 50 nM U50,488 [AID226664, Type: Literature]
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