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BioAssay: AID 620028

Activity of bovine eNOS 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)
 
 
Active(2)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(2)
 
 
Unspecified(1)
 
 
AID: 620028
Data Source: ChEMBL (770039)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Nitric oxide synthase, endothelial; AltName: Full=Constitutive NOS; Short=cNOS; AltName: Full=EC-NOS; AltName: Full=Endothelial NOS; Short=eNOS; AltName: Full=NOS type III; Short=NOSIII
Description ..   
Protein Family: NOS_oxygenase_euk
Comment ..   

Gene:NOS3     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 2
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)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
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
1Km*Km PubChem standard valueFloatμM
2Km activity commentKm activity commentString
3Km standard flagKm standard flagInteger
4Km qualifierKm qualifierString
5Km published valueKm published valueFloatμM
6Km standard valueKm standard valueFloatnM

* Activity Concentration.

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