CHEMBL2070953 (CID 53347902) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(7)
 
 
Unspecified(18)
 
 
Top Targets:
7TM GPCR Srsx(3)
 
 
CAP ED(2)
 
 
KCNQ channel(2)
 
 
SLC6sbd DAT1(1)
 
 
BioAssay Types:
Literature(23)
 
 
 
Confirmatory(2)
 
 
BioActivity Types:
EC50(5)
 
 
 
IC50(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 25    Data Row: 25   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID160686047]
EC50 0.26Activation of Kv7.1 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay [AID678686, Type: Literature]
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2
[SID126700205]
EC50 0.548SAR analysis for compounds that activate KCNQ1 potassium channels in the KCNQ1 expressing cells on automated patch clamp 2 [AID602121, Type: confirmatory]KCNQ1 gene product [Homo sapiens] [gi:32479527]
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3
[SID131536831]
EC50 0.72SAR analysis for compounds that activate KCNQ1 potassium channels in the KCNQ1 expressing cells on automated patch clamp III [AID602306, Type: confirmatory]KCNQ1 gene product [Homo sapiens] [gi:32479527]
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4
[SID160686047]
 Drug metabolism in human liver microsomes assessed as tolyl-oxidation by mass spectrophotometry [AID678685, Type: Literature]
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5
[SID160686047]
 Drug metabolism in rat liver microsomes assessed as tolyl-oxidation by mass spectrophotometry [AID678684, Type: Literature]
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6
[SID160686047]
 Drug metabolism in human liver microsomes assessed as methoxy-O-demethylation by mass spectrophotometry [AID678683, Type: Literature]
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7
[SID160686047]
 Drug metabolism in rat liver microsomes assessed as methoxy-O-demethylation by mass spectrophotometry [AID678705, Type: Literature]
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8
[SID160686047]
EC50 30Activation of KCNQ2 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control [AID678688, Type: Literature]
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9
[SID160686047]
EC50 30Activation of KCNQ4 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control [AID678689, Type: Literature]
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10
[SID160686047]
IC50 30Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay [AID678694, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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11
[SID160686047]
IC50 30Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay [AID678694, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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12
[SID160686047]
IC50 30Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay [AID678694, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
View
13
[SID160686047]
IC50 30Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay [AID678694, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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14
[SID160686047]
IC50 30Inhibition of human ERG expressed in CHO cells after 3 mins by patch clamp assay [AID678694, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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15
[SID160686047]
 Inhibition of human ERG at 10 uM [AID678698, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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16
[SID160686047]
 Inhibition of human ERG at 10 uM [AID678698, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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17
[SID160686047]
 Inhibition of human ERG at 10 uM [AID678698, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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18
[SID160686047]
 Inhibition of human ERG at 10 uM [AID678698, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
View
19
[SID160686047]
 Inhibition of human ERG at 10 uM [AID678698, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
View
20
[SID160686047]
 Activation of Kv7.1 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay relative to control [AID678687, Type: Literature]
View
21
[SID160686047]
 Inhibition of human DAT at 10 uM [AID678700, Type: Literature]Sodium-dependent dopamine transporter [gi:266667]
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22
[SID160686047]
 Inhibition of human DAT at 10 uM [AID678700, Type: Literature]Sodium-dependent dopamine transporter [gi:266667]
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23
[SID160686047]
 Inhibition of human DAT at 10 uM [AID678700, Type: Literature]Sodium-dependent dopamine transporter [gi:266667]
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24
[SID160686047]
 Inhibition of human DAT at 10 uM [AID678700, Type: Literature]Sodium-dependent dopamine transporter [gi:266667]
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25
[SID160686047]
 Selectivity ratio of EC50 for KCNQ2 channel to EC50 for Kv7.1 channel [AID678690, Type: Literature]
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26
[SID160686047]
 Selectivity ratio of EC50 for KCNQ4 channel to EC50 for Kv7.1 channel [AID678691, Type: Literature]
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27
[SID160686047]
 Activation of KCNQ2 channel expressed in CHO cells assessed as depolarization-induced thallium influx up to 30 uM after 3 mins by patch clamp assay relative to control [AID678692, Type: Literature]
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28
[SID160686047]
 Activation of KCNQ4 channel expressed in CHO cells assessed as depolarization-induced thallium influx up to 30 uM after 3 mins by patch clamp assay relative to control [AID678693, Type: Literature]
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29
[SID160686047]
 Fraction unbound in human plasma [AID678701, Type: Literature]
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30
[SID160686047]
 Fraction unbound in rat plasma [AID678702, Type: Literature]
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31
[SID160686047]
 Intrinsic clearance in human liver microsomes [AID678703, Type: Literature]
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32
[SID160686047]
 Intrinsic clearance in rat liver microsomes [AID678704, Type: Literature]
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33
[SID160686047]
 Inhibition of rat L-type calcium channel at 10 uM [AID678696, Type: Literature]
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34
[SID160686047]
 Inhibition of human adenosine A3 receptor at 10 uM [AID678695, Type: Literature]Adenosine receptor A [gi:1351831]
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35
[SID160686047]
 Inhibition of human adenosine A3 receptor at 10 uM [AID678695, Type: Literature]Adenosine receptor A [gi:1351831]
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36
[SID160686047]
 Inhibition of human CB1 receptor at 10 uM [AID678697, Type: Literature]Cannabinoid receptor 1 [gi:115562]
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37
[SID160686047]
 Inhibition of human CB1 receptor at 10 uM [AID678697, Type: Literature]Cannabinoid receptor 1 [gi:115562]
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38
[SID160686047]
 Inhibition of human CB1 receptor at 10 uM [AID678697, Type: Literature]Cannabinoid receptor 1 [gi:115562]
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39
[SID160686047]
 Inhibition of human 5HT2B receptor at 10 uM [AID678699, Type: Literature]5-hydroxytryptamine receptor 2B [gi:1168220]
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40
[SID160686047]
 Inhibition of human 5HT2B receptor at 10 uM [AID678699, Type: Literature]5-hydroxytryptamine receptor 2B [gi:1168220]
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41
[SID160686047]
 Inhibition of human 5HT2B receptor at 10 uM [AID678699, Type: Literature]5-hydroxytryptamine receptor 2B [gi:1168220]
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