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BioAssay: AID 619827

Inhibition of aminopeptidase N in human ES2 cells assessed as L-Leu-p-nitroanilide hydrolysis

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 muM) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 # 0.01 muM), 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)
 
 
AID: 619827
Data Source: ChEMBL (769838)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
Target
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     More BioActivity Data..
BioActive Compounds: 2
Description:
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 muM) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 # 0.01 muM), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.
(PMID: 21911297)
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

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM
11Inhibition activity commentInhibition activity commentString
12Inhibition standard flagInhibition standard flagInteger
13Inhibition qualifierInhibition qualifierString
14Inhibition published valueInhibition published valueFloat
15Inhibition standard valueInhibition standard valueFloat

* Activity Concentration.

Data Table (Concise)
Classification
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