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BioAssay: AID 468341

Inhibition of catalytic activity of human IRAP transfected in HEK293 cells assessed as formation of p-nitroaniline

The histidine residue in angiotensin IV was replaced by various conformationally constrained amino acids. The substitution of the His(4)-Pro(5) dipeptide sequence by the constrained Trp analogue Aia-Gly, in combination with beta(2)hVal substitution at the N-terminus, provided a new stable analogue H-(R)-beta(2)hVal-Tyr-Ile-Aia-Gly-Phe-OH (AL-40) that is a potent ligand for the Ang IV receptor IRAP and selective versus AP-N and the AT1 receptor. ..more
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Active(12)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Active(12)
 
 
AID: 468341
Data Source: ChEMBL (619204)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
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..
BioActive Compounds: 12
Description:
Title: The replacement of His(4) in angiotensin IV by conformationally constrained residues provides highly potent and selective analogues.

Abstract: The histidine residue in angiotensin IV was replaced by various conformationally constrained amino acids. The substitution of the His(4)-Pro(5) dipeptide sequence by the constrained Trp analogue Aia-Gly, in combination with beta(2)hVal substitution at the N-terminus, provided a new stable analogue H-(R)-beta(2)hVal-Tyr-Ile-Aia-Gly-Phe-OH (AL-40) that is a potent ligand for the Ang IV receptor IRAP and selective versus AP-N and the AT1 receptor.
(PMID: 19757839)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: HEK293

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Activity activity commentActivity activity commentString
7Activity standard flagActivity standard flagInteger
8Activity qualifierActivity qualifierString
9Activity published valueActivity published valueFloat
10Activity standard valueActivity standard valueFloat
11Ki activity commentKi activity commentString
12Ki standard flagKi standard flagInteger
13Ki qualifierKi qualifierString
14Ki published valueKi published valueFloat
15Ki standard valueKi standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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