Inhibition of aminopeptidase N in human ES2 cells assessed as L-Leu-p-nitroanilide hydrolysis - BioAssay Summary
A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. Within this series, compound 12h (IC(50)=6.28 ## 0.11 ##M) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 ## 0.01 ##M), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents. ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(2)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 619827
Data Source: ChEMBL (769838)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2013-05-15

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=Aminopeptidase N; Short=AP-N; Short=hAPN; AltName: Full=Alanyl aminopeptidase; AltName: Full=Aminopeptidase M; Short=AP-M; AltName: Full=Microsomal aminopeptidase; AltName: Full=Myeloid plasma membrane glycoprotein CD13; AltName: Full=gp150; AltName: CD_antigen=CD13
Description ..   
Protein Family: Peptidase M1 Aminopeptidase N family incudes tricorn interacting factor F3, Endoplasmic reticulum aminopeptidase 1 (ERAP1), Aminopeptidase Q (APQ)
Comment ..   

Gene:ANPEP     Related Protein 3D Structures
BioActive Compounds: 2
Description:
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Title: Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors.

Abstract: A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. Within this series, compound 12h (IC(50)=6.28 ## 0.11 ##M) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 ## 0.01 ##M), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.
(PMID: 21911297)
Comment
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Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 243

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4IC50 activity commentIC50 activity commentString
5IC50 standard flagIC50 standard flagInteger
6IC50 qualifierIC50 qualifierString
7IC50 published valueIC50 published valueFloatnM
8IC50 standard valueIC50 standard valueFloatnM
9Inhibition activity commentInhibition activity commentString
10Inhibition standard flagInhibition standard flagInteger
11Inhibition qualifierInhibition qualifierString
12Inhibition published valueInhibition published valueFloat
13Inhibition standard valueInhibition standard valueFloat
* Activity Concentration.

Data Table (Concise)
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Classification
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