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varenicline (CID 170361) - Compound BioActivity Data
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BioActivity Outcomes:
Active(69)
 
 
Inactive(15)
 
 
Inconclusive(11)
 
 
Unspecified(88)
 
 
Top Targets:
Neur chan LBD(117)
 
 
 
 
 
KAZAL SLC21(3)
 
 
Glutaminase(1)
 
 
MFS(1)
 
 
HpcH HpaI(1)
 
 
BioAssay Types:
Literature(174)
 
 
 
 
 
Confirmatory(9)
 
 
BioActivity Types:
Ki(45)
 
 
EC50(23)
 
 
 
IC50(18)
 
 
 
 
Potency(9)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 122    Data Row: 183   Total Pages: 4   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103471545]
Ki 5e-05Displacement of [3H]epibatidine from rat alpha4beta2 nACHR [AID700118, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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2
[SID103471545]
Ki 5e-05Displacement of [3H]epibatidine from rat alpha4beta2 nACHR [AID700118, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
3
[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]
View
4
[SID103471545]
Ki 6e-05Binding affinity to rat cortex Nicotinic acetylcholine receptor alpha4-beta2 using [3H]nicotine [AID254424, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
5
[SID103471545]
EC50 6e-05Partial agonist activity at alpha4beta 2 nAChR [AID675881, Type: Literature]
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6
[SID103471545]
Ki 6e-05Binding affinity to alpha4beta2 nAChR in rat cortex [AID726239, Type: Literature]
View
7
[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]
View
8
[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 alpha-4 [gi:1351848]
View
9
[SID103471545]
Ki 0.00012Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex [AID322331, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
10
[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]
View
11
[SID103471545]
Ki 0.00012Displacement of [3H]-Epibatidine from rat alpha4beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729084, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
12
[SID103471545]
Ki 0.00012Displacement of [3H]-Epibatidine from rat alpha4beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729084, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
View
13
[SID103471545]
Ki 0.00012Displacement of [3H]epibatidine from rat cerebral cortex alpha4beta2* nAChR incubated for 4 hrs by liquid scintillation assay [AID699417, Type: Literature]
View
14
[SID103471545]
Ki 0.000295Displacement of [3H]epibatidine from alpha4beta2 nicotinic receptor expressed in human HEK293 cells [AID495031, Type: Literature]
View
15
[SID103471545]
Ki 0.0004Binding affinity to alpha4beta2 nAChR [AID710166, Type: Literature]
View
16
[SID103471545]
Ki 0.00048Displacement of [3H]-Epibatidine from rat alpha2beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729088, Type: Literature]Neuronal acetylcholine receptor subunit alpha-2 [gi:2851491]
View
17
[SID103471545]
Ki 0.00048Displacement of [3H]-Epibatidine from rat alpha2beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729088, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
View
18
[SID103471545]
Ki 0.0025Displacement of [3H]-Epibatidine from rat alpha3beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729086, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
View
19
[SID103471545]
Ki 0.0025Displacement of [3H]-Epibatidine from rat alpha3beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729086, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
View
20
[SID103471545]
Ki 0.028Displacement of [3H]-Epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729083, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
View
21
[SID103471545]
Ki 0.028Displacement of [3H]-Epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729083, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
22
[SID103471545]
Ki 0.0325Displacement of [125I]iodoMLA from rat cerebral cortex alpha7 nAChR at 50 nM incubated for 2 hrs by microplate scintillation assay [AID699416, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:146345356]
View
23
[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]
View
24
[SID103471545]
Ki 0.037Displacement of [3H]-Epibatidine from rat alpha7 nACHR expressed in HEK293 cell membranes membranes by liquid scintillation counting analysis [AID729082, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:146345356]
View
25
[SID103471545]
IC50 0.0389Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting [AID710161, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:1351848]
View
26
[SID103471545]
IC50 0.0389Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting [AID710161, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
View
27
[SID103471545]
EC50 0.046Agonist activity at rat alpha6beta2 nAChR assessed as [3H]dopamine release by beta counting [AID629809, Type: Literature]
View
28
[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]
View
29
[SID103471545]
EC50 0.046Agonist activity at rat alpha4beta2 nAChR assessed as [3H]dopamine release by beta counting [AID629810, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
30
[SID103471545]
Ki 0.0747Displacement of [3H]epibatidine from alpha3beta4 nicotinic receptor expressed in human HEK293 cells [AID495033, Type: Literature]
View
31
[SID103471545]
Ki 0.086Displacement of [3H]epibatidine from rat alpha3beta4 nACHR [AID700117, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
View
32
[SID103471545]
Ki 0.086Binding affinity to alpha3beta4 nAChR [AID710167, Type: Literature]
View
33
[SID103471545]
Ki 0.086Displacement of [3H]epibatidine from rat alpha3beta4 nACHR [AID700117, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
View
34
[SID103471545]
Ki 0.089Displacement of [3H]epibatidine from alpha6/4beta4 nicotinic receptor expressed in human HEK293 cells [AID495034, Type: Literature]
View
35
[SID103471545]
IC50 0.094Desensitization of human alpha4beta2 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2 hrs by liquid scintillation counting analysis [AID729076, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:113105]
View
36
[SID103471545]
Ki 0.094Displacement of [3H]-Epibatidine from rat alpha2beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729087, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
View
37
[SID103471545]
IC50 0.094Desensitization of human alpha4beta2 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2 hrs by liquid scintillation counting analysis [AID729076, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:1351848]
View
38
[SID103471545]
Ki 0.094Displacement of [3H]-Epibatidine from rat alpha2beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729087, Type: Literature]Neuronal acetylcholine receptor subunit alpha-2 [gi:2851491]
View
39
[SID103471545]
Ki 0.11Displacement of [3H]epibatidine from rat alpha4beta4 nACHR [AID700120, Type: Literature]Neuronal acetylcholine receptor subunit alpha-4 [gi:8469182]
View
40
[SID103471545]
IC50 0.11Inhibition of human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay [AID700126, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:2506129]
View
41
[SID103471545]
Ki 0.11Displacement of [3H]epibatidine from rat alpha4beta4 nACHR [AID700120, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
View
42
[SID103471545]
Ki 0.11Binding affinity to alpha4beta4 nAChR [AID710165, Type: Literature]
View
43
[SID103471545]
IC50 0.11Inhibition of human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay [AID700126, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:254763435]
View
44
[SID103471545]
Ki 0.125Binding affinity to rat alpha7 nACHR at 10 uM [AID696713, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:146345356]
View
45
[SID103471545]
Ki 0.125Displacement of [3H]epibatidine from alpha7 nicotinic receptor expressed in human HEK293 cells [AID495035, Type: Literature]
View
46
[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]
View
47
[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 alpha-4 [gi:1351848]
View
48
[SID103471545]
Ki 0.3Binding affinity to rat alpha7 nAChR expressed in Xenopus laevis oocytes [AID705820, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:146345356]
View
49
[SID103471545]
Ki 0.39Displacement of [3H]-Epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729085, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
View
50
[SID103471545]
Ki 0.39Displacement of [3H]-Epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis [AID729085, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
View