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BioAssay: AID 329317

Inhibition of human recombinant IRAP expressed in HEK293 cells

Angiotensin IV, a metabolite of angiotensin II, inhibits the enzyme insulin regulated aminopeptidase or IRAP and also, although with lower potency, aminopeptidase-N (AP-N). When both beta (2)-homo amino acid- and beta (3)-homo amino acid substitutions were used, allowed the identification of H-( R)beta (2)hVal-Tyr-Ile-His-Pro-beta (3)hPhe-OH as a potent and stable Ang IV analog with high selectivity for IRAP versus AP-N and the AT1 receptor. ..more
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 Tested Compounds
 Tested Compounds
All(17)
 
 
Unspecified(17)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Unspecified(17)
 
 
 Related BioAssays
 Related BioAssays
AID: 329317
Data Source: ChEMBL (477343)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-08-23

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Leucyl-cystinyl aminopeptidase; Short=Cystinyl aminopeptidase; AltName: Full=Insulin-regulated membrane aminopeptidase; AltName: Full=Insulin-responsive aminopeptidase; Short=IRAP; AltName: Full=Oxytocinase; Short=OTase; AltName: Full=Placental leucine aminopeptidase; Short=P-LAP; Contains: RecName: Full=Leucyl-cystinyl aminopeptidase, pregnancy serum form
Description ..   
Protein Family: Peptidase M1 Aminopeptidase N family incudes tricorn interacting factor F3, Endoplasmic reticulum aminopeptidase 1 (ERAP1), Aminopeptidase Q (APQ)
Comment ..   

Gene:LNPEP     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Beta-homo-amino acid scan of angiotensin IV.

Abstract: Angiotensin IV, a metabolite of angiotensin II, inhibits the enzyme insulin regulated aminopeptidase or IRAP and also, although with lower potency, aminopeptidase-N (AP-N). When both beta (2)-homo amino acid- and beta (3)-homo amino acid substitutions were used, allowed the identification of H-( R)beta (2)hVal-Tyr-Ile-His-Pro-beta (3)hPhe-OH as a potent and stable Ang IV analog with high selectivity for IRAP versus AP-N and the AT1 receptor.
(PMID: 18386881)
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
BAO: Assay Format: cell-based format
Assay Cell Type: HEK293
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Log Ki activity commentLog Ki activity commentString
2Log Ki standard flagLog Ki standard flagInteger
3Log Ki qualifierLog Ki qualifierString
4Log Ki published valueLog Ki published valueFloat
5Log Ki standard valueLog Ki standard valueFloat

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