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BioAssay: AID 620027

Ratio of Kcat to Km for mouse iNOS by Michaelis-Menten equation analysis

A series of optically active stereoisomers of 3,4-methanoarginine (1-4 and ent-1-ent-4) with trans/cis, D/L, and syn/anti stereochemical diversity, the side-chains of which were restricted in various special arrangements, was designed as biologically useful arginine mimetics. These conformationally restricted arginine analogues were synthesized effectively by using a series of chiral more ..
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 620027
Data Source: ChEMBL (770038)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Nitric oxide synthase, inducible; AltName: Full=Inducible NO synthase; Short=Inducible NOS; Short=iNOS; AltName: Full=Macrophage NOS; Short=MAC-NOS; AltName: Full=NOS type II; AltName: Full=Peptidyl-cysteine S-nitrosylase NOS2
Description ..   
Protein Family: NOS_oxygenase_euk
Comment ..   

Gene:NOS2     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Synthesis of a series of 3,4-methanoarginines as side-chain conformationally restricted analogues of arginine.

Abstract: A series of optically active stereoisomers of 3,4-methanoarginine (1-4 and ent-1-ent-4) with trans/cis, D/L, and syn/anti stereochemical diversity, the side-chains of which were restricted in various special arrangements, was designed as biologically useful arginine mimetics. These conformationally restricted arginine analogues were synthesized effectively by using a series of chiral 3,4-methanoamino acid equivalents (7-10 and ent-7-ent-10) as the key synthetic units. Their biological evaluation with three isoforms of nitric oxide synthase showed that trans-3,4-methano-L-syn-arginine (2) was a good substrate, having close potency to L-arginine, and isoforms selectivities were also similar to those of l-arginine.
(PMID: 21917467)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kcat/Km activity commentKcat/Km activity commentString
2Kcat/Km standard flagKcat/Km standard flagInteger
3Kcat/Km qualifierKcat/Km qualifierString
4Kcat/Km published valueKcat/Km published valueFloat/s/mM
5Kcat/Km standard valueKcat/Km standard valueFloat/s/mM

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