Acetylcholine (CID 187) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(63)
 
 
Inactive(57)
 
 
Inconclusive(8)
 
 
Unspecified(104)
 
 
Top Targets:
Neur chan LBD(35)
 
 
 
 
Neur chan mem..(7)
 
 
 
NR LBD TR(4)
 
 
7TM GPCR Srx(4)
 
 
 
PolY Pol IV k..(3)
 
 
 
BioAssay Types:
Literature(160)
 
 
 
 
Confirmatory(56)
 
 
 
Screening(1)
 
 
BioActivity Types:
Potency(54)
 
 
 
EC50(38)
 
 
 
Ki(20)
 
 
 
 
IC50(19)
 
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 215    Data Row: 232   Total Pages: 5   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID104234160]
EC50 0.0011Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining [AID672151, Type: Literature]
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2
[SID104234160]
EC50 0.0011Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511592, Type: Literature]Muscarinic acetylcholine receptor M [gi:113118]
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3
[SID104234160]
EC50 0.0011Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511592, Type: Literature]Muscarinic acetylcholine receptor M [gi:113118]
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4
[SID104234160]
EC50 0.0012Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining [AID672153, Type: Literature]
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5
[SID104234160]
EC50 0.0012Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511603, Type: Literature]Muscarinic acetylcholine receptor M [gi:543761]
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6
[SID104234160]
EC50 0.0012Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511603, Type: Literature]Muscarinic acetylcholine receptor M [gi:543761]
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7
[SID104234160]
EC50 0.0012Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511603, Type: Literature]Muscarinic acetylcholine receptor M [gi:543761]
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8
[SID104234160]
EC50 0.0012Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511603, Type: Literature]Muscarinic acetylcholine receptor M [gi:543761]
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9
[SID104234160]
EC50 0.0032Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511597, Type: Literature]Muscarinic acetylcholine receptor M [gi:113125]
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10
[SID104234160]
EC50 0.0032Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511597, Type: Literature]Muscarinic acetylcholine receptor M [gi:113125]
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11
[SID104234160]
EC50 0.0032Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511597, Type: Literature]Muscarinic acetylcholine receptor M [gi:113125]
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12
[SID104234160]
EC50 0.0032Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511597, Type: Literature]Muscarinic acetylcholine receptor M [gi:113125]
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13
[SID104234160]
EC50 0.0032Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511597, Type: Literature]Muscarinic acetylcholine receptor M [gi:113125]
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14
[SID104234160]
EC50 0.0032Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining [AID672157, Type: Literature]
View
15
[SID104234160]
Ki 0.0076Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates [AID239589, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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16
[SID104234160]
EC50 0.01Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511600, Type: Literature]Muscarinic acetylcholine receptor M [gi:23503039]
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17
[SID104234160]
EC50 0.01Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511600, Type: Literature]Muscarinic acetylcholine receptor M [gi:23503039]
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18
[SID104234160]
EC50 0.01Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511600, Type: Literature]Muscarinic acetylcholine receptor M [gi:23503039]
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19
[SID104234160]
EC50 0.01Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining [AID672155, Type: Literature]
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20
[SID104234160]
Ki 0.011Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand [AID145983, Type: Literature]Neuronal acetylcholine receptor subunit alpha-2 [gi:2851491]
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21
[SID104234160]
IC50 0.012In vitro ability to displace [3H]oxotremorine-M (OXO-M) from rat cerebral cortex muscarinic receptor. [AID141531, Type: Literature]
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22
[SID104234160]
IC50 0.012Compound was tested in vitro for its binding affinity to muscarinic acetylcholine receptor from rat cortical homogenates using [3H]OXO-M as radioligand [AID141545, Type: Literature]
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23
[SID104234160]
IC50 0.012The compound was tested in vitro for central muscarinic acetylcholine receptor affinity to displace [3H]oxotremorine-M from rat cerebral cortex; Value ranges from 7-20 [AID141812, Type: Literature]
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24
[SID104234160]
Ki 0.0377Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 3 hrs [AID536863, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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25
[SID104234160]
Ki 0.039Displacement of [3H]cystisine from nicotinic alpha-4-beta-2 receptor in rat brain [AID320061, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
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26
[SID104234160]
Ki 0.041Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand [AID146006, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
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27
[SID104234160]
Ki 0.043Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand [AID145685, Type: Literature]
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28
[SID104234160]
Ki 0.045Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand [AID146486, Type: Literature]Neuronal acetylcholine receptor subunit beta-2 [gi:6226548]
View
29
[SID104234160]
Ki 0.083Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand [AID146772, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
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30
[SID104234160]
Ki 0.085Displacement of [3H]oxotremorine from muscarinic receptor in rat brain [AID320063, Type: Literature]
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31
[SID104234160]
Ki 0.18Binding affinity towards rat alpha2-beta4 nACh receptor expressed in HEK293 cells using [3H]EB as radioligand [AID225720, Type: Literature]Neuronal acetylcholine receptor subunit beta-4 [gi:113111]
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32
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining [AID672159, Type: Literature]
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33
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511594, Type: Literature]Muscarinic acetylcholine receptor M [gi:113122]
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34
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511594, Type: Literature]Muscarinic acetylcholine receptor M [gi:113122]
View
35
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511594, Type: Literature]Muscarinic acetylcholine receptor M [gi:113122]
View
36
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511594, Type: Literature]Muscarinic acetylcholine receptor M [gi:113122]
View
37
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511594, Type: Literature]Muscarinic acetylcholine receptor M [gi:113122]
View
38
[SID104234160]
EC50 0.22Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay [AID511594, Type: Literature]Muscarinic acetylcholine receptor M [gi:113122]
View
39
[SID104234160]
Ki 0.62Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs [AID536862, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
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40
[SID104234160]
EC50 0.63Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells. [AID142144, Type: Literature]
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41
[SID104234160]
Ki 0.82Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand [AID146162, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
View
42
[SID104234160]
Ki 0.881Displacement of [3H]epibatidine from Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates [AID239611, Type: Literature]Neuronal acetylcholine receptor subunit alpha-3 [gi:113061]
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43
[SID104234160]
IC50 1Vasorelaxant activity in Wistar rat endothelium-intact aortic rings assessed as inhibition of phenylephrine-induced contractions after 10 to 30 mins [AID602907, Type: Literature]
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44
[SID104234160]
IC50 1Vasorelaxant activity in Wistar rat endothelium-intact thoracic aortic ring assessed as inhibition of phenylephrine-induced contraction measured after 60 mins [AID662198, Type: Literature]
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45
[SID104234160]
EC50 3.12Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells assessed as calcium influx measured every 1 sec for 1 min followed by every 30 secs for 10 mins by FLIPR assay [AID684908, Type: Literature]
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46
[SID104234160]
Ki 3.16228Displacement of [125I]alpha-bungarotoxin from Lymnaea stagnalis His-tagged AchBP [AID415528, Type: Literature]Acetylcholine-binding protein [gi:14285341]
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47
[SID104234160]
Ki 3.509Displacement of [3H]alpha-bungaro-toxine from nicotinic alpha-7 receptor in rat brain [AID320062, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:146345356]
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48
[SID104234160]
EC50 5Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype TE671 (muscle) [AID145357, Type: Literature]
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49
[SID104234160]
Ki 6.30957Displacement of [3H]-epibatidine from histidine-tagged Lymnaea stagnalis AChBP expressed in Sf9 cells after 1.5 hrs by liquid scintillation counting [AID620032, Type: Literature]Acetylcholine-binding protein [gi:14285341]
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50
[SID104234160]
Ki 7.94328Displacement of [3H]-MLA from human alpha7 nAChR expressed in human SH-SY5Y cells after 1.5 hrs by liquid scintillation counting [AID620034, Type: Literature]Neuronal acetylcholine receptor subunit alpha-7 [gi:2506127]
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