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Idazoxan (CID 54459) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(100)
 
 
Inactive(195)
 
 
Inconclusive(66)
 
 
Unspecified(114)
 
 
Top Targets:
7TM GPCR Srx(41)
 
 
 
 
 
7TM GPCR Srsx(9)
 
 
 
NR LBD PPAR(8)
 
 
 
 
NR LBD AR(7)
 
 
 
 
NR LBD ER(7)
 
 
 
BioAssay Types:
Literature(252)
 
 
 
 
 
Confirmatory(179)
 
 
 
 
Summary(24)
 
 
 
 
Screening(11)
 
 
BioActivity Types:
Potency(193)
 
 
 
 
Kd(33)
 
 
Ki(28)
 
 
IC50(13)
 
 
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 370    Data Row: 475   Total Pages: 10   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103169925]
Ki 0.0015Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand [AID35902, Type: Literature]
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2
[SID103169925]
Ki 0.00172In vitro binding affinity at Alpha-2 adrenergic receptor in rat cortex by radioligand binding assay using [3H]rauwolscine [AID37375, Type: other]
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3
[SID103169925]
Kd 0.00229Alpha-2 adrenergic receptor antagonist activity in a rat vas deferens assay. Values ranges from 8.38-8.64 [AID35349, Type: Literature]
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4
[SID103169925]
Kd 0.00275Alpha-2 adrenergic receptor pA2 value against clonidine in vitro experiment in rat vas deferens [AID35340, Type: Literature]
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5
[SID103169925]
Kd 0.00398In vitro reversal of inhibitory effect of UK - 14304 on the contractile response of guinea pig ileum to field stimulation. [AID79507, Type: Literature]
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6
[SID103169925]
Kd 0.00398Ability to reverse inhibitory effects of UK-14304 on the contraction of guinea pig ileum as a measure of alpha-2 adrenergic receptor antagonism. [AID80588, Type: Literature]
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7
[SID103169925]
Ki 0.00427Binding affinity to I2 imidazoline binding site [AID650486, Type: Literature]
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8
[SID103169925]
Kd 0.00513Antagonist potency towards alpha-2 adrenergic receptor in the rat electrically stimulated vas deferens with reference to P-aminoclonidine [AID35357, Type: Literature]
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9
[SID103169925]
Ki 0.00708Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting [AID650481, Type: Literature]Alpha-2A adrenergic receptor [gi:1351829]
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10
[SID103169925]
Ki 0.00708Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells [AID339888, Type: Literature]Alpha-2A adrenergic receptor [gi:1351829]
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11
[SID103169925]
Kd 0.00776Alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs clonidin [AID35479, Type: Literature]
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12
[SID103169925]
Kd 0.00776In vitro antagonistic activity against alpha-2 adrenergic receptor in isolated electrically stimulated rat vas deferens (clonidine-induced decrease in twitch height) [AID35366, Type: Literature]
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13
[SID103169925]
Kd 0.00776In vitro antagonistic activity against alpha-2 adrenergic receptor in isolated electrically stimulated rat vas deferens (clonidine-induced decrease in twitch height) [AID218809, Type: Literature]
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14
[SID103169925]
Ki 0.008Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells [AID306189, Type: Literature]
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15
[SID103169925]
IC50 0.00832Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. [AID36067, Type: Literature]
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16
[SID103169925]
Kd 0.00851Antagonistic activity against presynaptic alpha-2 adrenergic receptor in isolated rat vas deferens using xylazine as agonist [AID35361, Type: Literature]
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17
[SID103169925]
Kd 0.00912Antagonism of rat alpha-2 adrenergic receptor from rat vas deferens [AID35199, Type: Literature]
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18
[SID103169925]
Kd 0.00912Antagonistic activity against alpha-2 adrenergic receptor in rat vas deferens [AID35360, Type: Literature]
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19
[SID103169925]
Kd 0.00977Tested for the alpha-2-adrenoreceptor blocking activity by antagonism of clonidine-induced depression of the twitch responses of the field-stimulated prostatic portion of isolated rat vas deferens [AID219799, Type: Literature]Alpha-2C adrenergic receptor [gi:231464]
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20
[SID103169925]
Kd 0.00977Tested for the alpha-2-adrenoreceptor blocking activity by antagonism of clonidine-induced depression of the twitch responses of the field-stimulated prostatic portion of isolated rat vas deferens [AID219799, Type: Literature]Alpha-2A adrenergic receptor [gi:231461]
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21
[SID103169925]
Kd 0.00977Tested for the alpha-2-adrenoreceptor blocking activity by antagonism of clonidine-induced depression of the twitch responses of the field-stimulated prostatic portion of isolated rat vas deferens [AID219799, Type: Literature]Alpha-2B adrenergic receptor [gi:47117345]
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22
[SID103169925]
Ki 0.01Binding affinity for imidazoline receptor I-2 [AID223241, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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23
[SID103169925]
Ki 0.01Binding affinity for imidazoline receptor I-2 [AID223241, Type: Literature]Amine oxidase [flavin-containing] B [gi:113980]
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24
[SID103169925]
Ki 0.01Ability to displace [3H]-clonidine from alpha-1 adrenergic receptor in rat brain homogenates in vitro [AID36946, Type: Literature]
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25
[SID103169925]
Ki 0.01Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]clonidine from rat brain cortical membranes [AID37078, Type: Literature]
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26
[SID103169925]
Ki 0.01Ability to displace [3H]clonidine from alpha-2 adrenergic receptor in rat brain homogenates in vitro [AID218806, Type: Literature]
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27
[SID103169925]
Kd 0.01047Antagonist potency for alpha 2 adrenoceptor [AID196665, Type: Literature]
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28
[SID103169925]
Kd 0.01175Evaluated for its presynaptic Alpha-2 adrenergic receptor antagonistic activity against rat vas deferens using clonidine as the control expressed as slope [AID35365, Type: other]
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29
[SID103169925]
Ki 0.01778Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells [AID339896, Type: Literature]Alpha-2C adrenergic receptor [gi:20141211]
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30
[SID103169925]
Ki 0.01778Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting [AID650476, Type: Literature]Alpha-2C adrenergic receptor [gi:20141211]
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31
[SID103169925]
Kd 0.01862Presynaptic antagonistic activity against alpha-2 adrenergic receptor from rat, isolated, field-stimulated vas deferens, using clonidine as the agonist [AID35476, Type: Literature]
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32
[SID103169925]
Ki 0.019Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells [AID306191, Type: Literature]
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33
[SID103169925]
IC50 0.0195Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. [AID35399, Type: Literature]
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34
[SID103169925]
IC50 0.021In vitro inhibition of binding of [3H]-RX-821002 to alpha-2 adrenergic receptor site in rat brain membranes. [AID36918, Type: Literature]
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35
[SID103169925]
Ki 0.02291Displacement of [3H]RX821002 from human alpha2B adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting [AID650477, Type: Literature]Alpha-2B adrenergic receptor [gi:27151763]
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36
[SID103169925]
Ki 0.02291Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2B receptor expressed in CHO cells [AID339892, Type: Literature]Alpha-2B adrenergic receptor [gi:27151763]
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37
[SID103169925]
Ki 0.028Displacement of [3H]2-BFI (1 nM) from imidazoline receptor I-2 in human brain [AID223240, Type: Literature]Amine oxidase [flavin-containing] B [gi:113980]
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38
[SID103169925]
Ki 0.028Displacement of [3H]2-BFI (1 nM) from imidazoline receptor I-2 in human brain [AID223240, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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39
[SID103169925]
Kd 0.03236Antagonistic activity against adrenergic alpha-2 receptor in longitudinal muscle strip of the guinea pig ileum using l-norepinephrine as agonist [AID36057, Type: Literature]Alpha-2A adrenergic receptor [gi:231461]
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40
[SID103169925]
Kd 0.03236Antagonistic activity against adrenergic alpha-2 receptor in longitudinal muscle strip of the guinea pig ileum using l-norepinephrine as agonist [AID36057, Type: Literature]Alpha-2C adrenergic receptor [gi:231464]
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41
[SID103169925]
Kd 0.03236Antagonistic activity against adrenergic alpha-2 receptor in longitudinal muscle strip of the guinea pig ileum using l-norepinephrine as agonist [AID36057, Type: Literature]Alpha-2B adrenergic receptor [gi:47117345]
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42
[SID103169925]
Kd 0.0389Antagonistic activity against longitudinal muscle strip of the guinea pig ileum using xylazine as agonist [AID36058, Type: Literature]
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43
[SID103169925]
Ki 0.05129Displacement of [3H]RX821002 from alpha2 adrenoceptor in human prefrontal cortex neural membrane [AID364880, Type: Literature]
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44
[SID103169925]
Ki 0.05129Displacement of [3H]RX821002 from alpha2 adrenergic receptor in human brain prefrontal cortex tissue by liquid scintillation spectrometry [AID404330, Type: Literature]
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45
[SID103169925]
Kd 0.05248Evaluated for its postsynaptic Alpha-2 adrenergic receptor antagonist activity against dog saphenous vein using norepinephrine as the control expressed as slope [AID36041, Type: other]
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46
[SID103169925]
IC50 0.0537Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. [AID36530, Type: Literature]
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47
[SID103169925]
Ki 0.089Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells [AID342860, Type: Literature]
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48
[SID103169925]
Ki 0.1Displacement of [3H]MK912 from adrenergic alpha-2B receptor expressed in COS7 cells [AID306190, Type: Literature]
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49
[SID103169925]
Kd 0.14125Antagonistic activity against postsynptic alpha-1 adrenergic receptor in rabbit pulmonary artery using l-norepinephrine as agonist [AID36281, Type: Literature]
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50
[SID103169925]
Ki 0.261Ability to displace [3H]prazosin from alpha-1 adrenergic receptor in rat brain homogenates in vitro [AID37169, Type: Literature]
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