NCGC00181133-02 (CID 16051933) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(5)
 
 
Inactive(4)
 
 
Unspecified(16)
 
 
Top Targets:
DUF1856(2)
 
 
 
BioAssay Types:
Literature(21)
 
 
 
Screening(2)
 
 
Confirmatory(2)
 
 
BioActivity Types:
Ki(4)
 
 
Potency(2)
 
 
Kd(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
[SID103505993]
Ki 0.0002Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in At-T20 cells [AID277898, Type: Literature]Vasopressin V1b receptor [gi:1351393]
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2
[SID103505993]
Ki 0.0008Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes [AID277899, Type: Literature]Vasopressin V2 receptor [gi:465020]
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3
[SID103505993]
Ki 0.00097Displacement of [3H]AVP from rat OT receptor expressed in CHO cells [AID277901, Type: Literature]Oxytocin receptor [gi:18269702]
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4
[SID103505993]
Ki 0.0108Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane [AID277900, Type: Literature]Vasopressin V1a receptor [gi:108935913]
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5
[SID103505993]
Kd Activity at OT receptor assessed as oxytocic activity in absence of magnesium [AID277897, Type: Literature]Oxytocin receptor [gi:143811431]
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6
[SID103505993]
Kd Activity at OT receptor assessed as oxytocic activity in absence of magnesium [AID277897, Type: Literature]Oxytocin receptor [gi:143811431]
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7
[SID103505993]
Kd Activity at OT receptor assessed as oxytocic activity in absence of magnesium [AID277897, Type: Literature]Oxytocin receptor [gi:143811431]
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8
[SID103505993]
 Agonist activity at vasopressin V1a receptor in phenoxybenzamine-treated Wistar rat uterus assessed as arteial vasopressor activity [AID426916, Type: Literature]Vasopressin V1a receptor [gi:108935913]
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9
[SID103505993]
 Selectivity index, Ki for rat V1b receptor/Ki for rat V2 receptor [AID277902, Type: Literature]Vasopressin V2 receptor [gi:465020]
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10
[SID103505993]
 Agonist activity at oxytocin receptor in Wistar rat uterus assessed as uterotonic activity in absence of Mg2+ [AID426914, Type: Literature]Oxytocin receptor [gi:18269702]
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11
[SID103505993]
 Selectivity index, Ki for rat V1b receptor/Ki for rat V1a receptor [AID277903, Type: Literature]Vasopressin V1b receptor [gi:1351393]
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12
[SID103505993]
 In vivo antidiuretic activity in female Sprague-Dawley rats by intraperitoneal administration using Vasopressin house standard (561 IU/mg) [AID190220, Type: Literature]
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13
[SID103505993]
 Antidiuretic activity in rat [AID277895, Type: Literature]
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14
[SID103505993]
 Vasopressor activity in rat [AID277896, Type: Literature]
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15
[SID103505993]
 Antidiuretic activity in fasted and hydrated Wistar rat assessed as compound required to yield antidiuresis time of 60 mins required for urinary excretion of half the water load at 0.001 to 100 nmol/kg, sc administered immediately after water loading by modified Burn test [AID426920, Type: Literature]
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16
[SID103505993]
 Antidiuretic activity in fasted and hydrated Wistar rat assessed as compound potency to yield antidiuresis time of 60 mins required for urinary excretion of half the water load at 0.001 to 100 nmol/kg, sc administered immediately after water loading by modified Burn test relative to 1-deamino-8-D-arginine vasopressin [AID426922, Type: Literature]
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17
[SID103505993]
 Antidiuretic activity in fasted and hydrated Wistar rat assessed as compound potency to yield antidiuresis time of 200 mins required for urinary excretion of half the water load at 0.001 to 100 nmol/kg, sc administered immediately after water loading by modified Burn test relative to 1-deamino-8-D-arginine vasopressin [AID426923, Type: Literature]
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18
[SID103505993]
 Volume of distribution at steady state in human after iv administration [AID540209, Type: Literature]
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19
[SID103505993]
 Clearance in human after iv administration [AID540210, Type: Literature]
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20
[SID103505993]
 Mean residence time in human after iv administration [AID540212, Type: Literature]
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21
[SID103505993]
 Half life in human after iv administration [AID540213, Type: Literature]
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22
[SID103505993]
 Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis [AID592681, Type: Literature]
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23
[SID103505993]
 Selectivity index, Ki for rat V1b receptor/Ki for rat OT receptor [AID277904, Type: Literature]
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24
[SID144206930]
 qHTS of D3 Dopamine Receptor Potentiators: qHTS [AID652051, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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25
[SID144206930]
 qHTS of D3 Dopamine Receptor Potentiators: qHTS [AID652051, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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26
[SID144206930]
 qHTS of D3 Dopamine Receptor Potentiators: qHTS [AID652051, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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27
[SID144206930]
 qHTS of D3 Dopamine Receptor Potentiators: qHTS [AID652051, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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28
[SID144206930]
 qHTS of D3 Dopamine Receptor Agonist: qHTS [AID652048, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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29
[SID144206930]
 qHTS of D3 Dopamine Receptor Agonist: qHTS [AID652048, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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30
[SID144206930]
 qHTS of D3 Dopamine Receptor Agonist: qHTS [AID652048, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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31
[SID144206930]
 qHTS of D3 Dopamine Receptor Agonist: qHTS [AID652048, Type: screening]DRD3 gene product [Homo sapiens] [gi:89191863]
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32
[SID144206930]
Potency qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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33
[SID144206930]
Potency qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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34
[SID144206930]
Potency qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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35
[SID144206930]
Potency qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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36
[SID144206930]
Potency qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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37
[SID144206930]
Potency qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
View