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BioAssay: AID 647502

Inhibition of human CYP2C9

Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic profiles. These designs were applied in the identification of gamma-secretase modulators leading to highly efficacious agents for reduction of central nervous system Abeta(42) in various animal models. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 647502
Data Source: ChEMBL (804950)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Cytochrome P450 2C9; AltName: Full=(R)-limonene 6-monooxygenase; AltName: Full=(S)-limonene 6-monooxygenase; AltName: Full=(S)-limonene 7-monooxygenase; AltName: Full=CYPIIC9; AltName: Full=Cytochrome P-450MP; AltName: Full=Cytochrome P450 MP-4; AltName: Full=Cytochrome P450 MP-8; AltName: Full=Cytochrome P450 PB-1; AltName: Full=S-mephenytoin 4-hydroxylase
Description ..   
Protein Family: Cytochrome P450
Comment ..   

Gene:CYP2C9     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Description:
Title: Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious gamma-secretase modulators in vivo.

Abstract: Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic profiles. These designs were applied in the identification of gamma-secretase modulators leading to highly efficacious agents for reduction of central nervous system Abeta(42) in various animal models.
(PMID: 22098494)
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View All Data
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