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BioAssay: AID 68159

Evaluation as substrate of endothelial nitric oxide synthase by hemoglobin assay using NOHA as control

Because of the double-edged nature of NO, the development of isoform-selective NOS substrates is a highly desirable goal. Given the striking similarity in the heme active sites of the three NOS isoforms, it presents an challenging problem. Several N-aryl-N'-hydroxyguanidines have recently been shown as substrates that are selective for iNOS over nNOS. Here, we report the first success that 3 is a good substrate for nNOS (70% activity of NOHA, K(m) approximately 40 +/- 6 microM) over iNOS. ..more
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Unspecified(18)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Unspecified(18)
 
 
 Related BioAssays
 Related BioAssays
AID: 68159
Data Source: ChEMBL (65321)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: Isoform-selective substrates of nitric oxide synthase.

Abstract: Because of the double-edged nature of NO, the development of isoform-selective NOS substrates is a highly desirable goal. Given the striking similarity in the heme active sites of the three NOS isoforms, it presents an challenging problem. Several N-aryl-N'-hydroxyguanidines have recently been shown as substrates that are selective for iNOS over nNOS. Here, we report the first success that 3 is a good substrate for nNOS (70% activity of NOHA, K(m) approximately 40 +/- 6 microM) over iNOS.
(PMID: 12773030)
Comment
Putative Target:

ChEMBL Target ID: 11573
Target Type: SINGLE PROTEIN
Pref Name: Nitric-oxide synthase, endothelial
Synonyms: cNOS;Constitutive NOS;EC-NOS;Endothelial NOS;eNOS;Nitric oxide synthase; endothelial;NOS type III;NOSIII;
Gene Name: NOS3;
Protein Accession: P29474;
Protein GI: 266648;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: enzyme
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1NO formation activity commentNO formation activity commentString
2NO formation standard flagNO formation standard flagInteger
3NO formation qualifierNO formation qualifierString
4NO formation published valueNO formation published valueFloat%
5NO formation standard valueNO formation standard valueFloat%

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