1-((1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl)acetyl)piperidine-4-acetic acid (CID 9874248) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(2)
 
 
Unspecified(11)
 
 
Top Targets:
Trans IPPS HH(1)
 
 
BioAssay Types:
Literature(13)
 
 
 
BioActivity Types:
IC50(2)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 13    Data Row: 13   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103382167]
IC50 0.078Inhibition of squalene synthase from human hepatoma cells (HepG2) [AID227678, Type: Literature]Squalene synthase [gi:585126]
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2
[SID103382167]
IC50 0.213Inhibition of recombinant squalene synthase assessed as conversion of trans,trans-[1-3H]farnesyl pyrophosphate to [3H]squalene after 10 mins by liquid scintillation counting [AID598881, Type: Literature]
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3
[SID103382167]
 Stability in human liver microsomes assessed as compound remaining after 60 mins [AID598882, Type: Literature]
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4
[SID103382167]
 In vivo inhibition of squalene synthase in NMRI rat assessed as inhibition of hepatic [14C]cholesterol biosynthesis at 3 mg/kg, po measured after 1 hr by liquid scintillation counting [AID598883, Type: Literature]
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5
[SID103382167]
 In vivo inhibition of squalene synthase in NMRI rat assessed as inhibition of hepatic [14C]cholesterol biosynthesis at 1 mg/kg, po measured after 1 hr by liquid scintillation counting [AID598884, Type: Literature]
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6
[SID103382167]
 Lipid lowering effect in marmosets assessed as reduction in plasma total cholesterol level at 100 mg/kg, po administered once daily for 7 days [AID672685, Type: Literature]
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7
[SID103382167]
 Lipid lowering effect in marmosets assessed as reduction in plasma HDL-cholesterol level at 100 mg/kg, po administered once daily for 7 days [AID672686, Type: Literature]
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8
[SID103382167]
 Lipid lowering effect in marmosets assessed as reduction in plasma non HDL-cholesterol level at 100 mg/kg, po administered once daily for 7 days [AID672687, Type: Literature]
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9
[SID103382167]
 Lipid lowering effect in marmosets assessed as reduction in plasma triglyceride level at 100 mg/kg, po administered once daily for 7 days [AID672688, Type: Literature]
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10
[SID103382167]
 Compound at a dose of 3 mg/kg was dministered orally to 6 week old male Wistar rats and was evaluated for the inhibition of terol synthesis [AID219414, Type: Literature]
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11
[SID103382167]
 In vivo inhibition of sterol synthesis in rats following 10 mg/kg p.o. [AID219412, Type: Literature]
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12
[SID103382167]
 Compound at a dose of 1 mg/kg was administered orally to 6 week old male Wistar rats and was evaluated for the inhibition of sterol synthesis [AID219411, Type: Literature]
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13
[SID103382167]
 Concentration required for 50% inhibitory activity against cholesterol synthesis in rat liver [AID219271, Type: Literature]
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