varenicline (CID 170361) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(16)
 
 
Inactive(7)
 
 
Unspecified(26)
 
 
Top Targets:
Neur chan LBD(11)
 
 
 
Firefly Luc l..(1)
 
 
Glutaminase(1)
 
 
HpcH HpaI(1)
 
 
MFS(1)
 
 
BioAssay Types:
Literature(44)
 
 
 
 
Confirmatory(5)
 
 
BioActivity Types:
Ki(12)
 
 
Potency(5)
 
 
EC50(3)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 49    Data Row: 49   Total Pages: 1   
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103471545]
EC50 6e-05Partial agonist activity at alpha4beta 2 nAChR [AID675881, Type: Literature]
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2
[SID103471545]
Ki 6e-05Binding affinity to rat cortex Nicotinic acetylcholine receptor alpha4-beta2 using [3H]nicotine [AID254424, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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3
[SID103471545]
Ki 0.00011Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotine [AID254476, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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4
[SID103471545]
Ki 0.00011Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotine [AID254476, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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5
[SID103471545]
Ki 0.00012Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex [AID322331, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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6
[SID103471545]
Ki 0.000295Displacement of [3H]epibatidine from alpha4beta2 nicotinic receptor expressed in human HEK293 cells [AID495031, Type: Literature]
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7
[SID103471545]
Ki 0.0325Displacement of [125I]iodoMLA from alpha-7 nAChR in rat cerebral cortex [AID322332, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:146345356]
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8
[SID103471545]
EC50 0.046Agonist activity at rat alpha4beta2 nAChR assessed as [3H]dopamine release by beta counting [AID629810, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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9
[SID103471545]
EC50 0.046Agonist activity at rat alpha6beta2 nAChR assessed as [3H]dopamine release by beta counting [AID629809, Type: Literature]
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10
[SID103471545]
Ki 0.0747Displacement of [3H]epibatidine from alpha3beta4 nicotinic receptor expressed in human HEK293 cells [AID495033, Type: Literature]
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11
[SID103471545]
Ki 0.089Displacement of [3H]epibatidine from alpha6/4beta4 nicotinic receptor expressed in human HEK293 cells [AID495034, Type: Literature]
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12
[SID103471545]
Ki 0.125Displacement of [3H]epibatidine from alpha7 nicotinic receptor expressed in human HEK293 cells [AID495035, Type: Literature]
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13
[SID103471545]
Ki 0.24Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]epibatidine [AID254479, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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14
[SID103471545]
Ki 0.24Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]epibatidine [AID254479, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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15
[SID103471545]
Ki 0.617Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]alpha-bungarotoxin [AID254496, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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16
[SID103471545]
Ki 0.617Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in IMR32 cells using [3H]alpha-bungarotoxin [AID254496, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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17
[SID103471545]
Ki 3.54Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]alpha-bungarotoxin [AID254500, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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18
[SID103471545]
Ki 3.54Binding affinity to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]alpha-bungarotoxin [AID254500, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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19
[SID103471545]
Ki 8.2Binding affinity to alpha-1-beta-gamma-delta nicotinic receptor [AID495032, Type: Literature]
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20
[SID103856895]
 Wombat Data for BeliefDocking [AID493017, Type: Literature] [geneid:1134]
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21
[SID103856895]
 Wombat Data for BeliefDocking [AID493017, Type: Literature] [geneid:1134]
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22
[SID103856895]
 Wombat Data for BeliefDocking [AID493017, Type: Literature] [geneid:1134]
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23
[SID103471545]
 Agonist activity at rat alpha4beta2 nAChR assessed as [3H]dopamine release from rat striatum by beta counting relative to 10 uM nicotine [AID629808, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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24
[SID103471545]
 Substrates of transporters of clinical importance in the absorption and dispostion of drugs, OCT2 [AID588966, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
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25
[SID103471545]
 Antinociceptive activity in acute pain mouse model at 10 mg/kg, sc by tail flick method [AID322335, Type: Literature]
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26
[SID103471545]
 Antinociceptive activity in acute pain mouse model at 10 mg/kg, sc by hot plate method [AID322340, Type: Literature]
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27
[SID103471545]
 Antinociceptive activity in sc dosed mouse assessed as inhibition of nicotin induced hypothermia [AID322347, Type: Literature]
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28
[SID103471545]
 Effect on rectal temperature in mouse at 10000 mg/kg, sc [AID322350, Type: Literature]
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29
[SID103471545]
 Effect on locomotor activity in sc dosed mouse assessed as spontaneous activity [AID322358, Type: Literature]
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30
[SID103471545]
 Inhibition of nicotine-induced antinociception in sc dosed acute pain mouse model by tail flick method [AID322360, Type: Literature]
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31
[SID103471545]
 Inhibition of nicotine-induced antinociception in sc dosed acute pain mouse model by hot plate method [AID322361, Type: Literature]
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32
[SID103471545]
 Efficacy against human Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes at 10 uM relative to 10 uM nicotine [AID256206, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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33
[SID103471545]
 Efficacy against human Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes at 10 uM relative to 10 uM nicotine [AID256206, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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34
[SID103471545]
 Percent inhibition against 10 uM nicotine binding to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes at 10 uM [AID256387, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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35
[SID103471545]
 Percent inhibition against 10 uM nicotine binding to human Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes at 10 uM [AID256387, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
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36
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia [AID625279, Type: Literature]
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37
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis [AID625280, Type: Literature]
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38
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis [AID625281, Type: Literature]
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39
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis [AID625282, Type: Literature]
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40
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests [AID625283, Type: Literature]
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41
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure [AID625284, Type: Literature]
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42
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis [AID625285, Type: Literature]
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43
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis [AID625286, Type: Literature]
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44
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly [AID625287, Type: Literature]
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45
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice [AID625288, Type: Literature]
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46
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease [AID625289, Type: Literature]
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47
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty [AID625290, Type: Literature]
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48
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal [AID625291, Type: Literature]
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49
[SID103471545]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score [AID625292, Type: Literature]
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50
[SID103471545]
 Agonist activity at rat alpha6beta2 nAChR assessed as [3H]dopamine release from rat striatum by beta counting relative to 10 uM nicotine [AID629902, Type: Literature]
View