Inhibition of APN in human HL60 cells assessed as hydrolysis of L-Leu-p-nitroanilide by spectrophotometry - BioAssay Summary
Aminopeptidase N (APN) is involved in different physiological and pathological processes of tumor cells, including proliferation, invasion, apoptosis and metastasis. Herein one series of compounds derived from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol have been designed and synthesized. Furthermore, preliminary activity evaluation showed that some compounds elicited moderate inhibitory activity against APN with compounds 10e (IC(50)=6.1##0.5 ##M) possessing the best efficacy, which could be used as the lead compound in the future for anticancer agents research. ..more
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 Tested Compounds
 Tested Compounds
All(6)
 
 
Active(2)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Active(2)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 613980
Data Source: ChEMBL (763991)
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: Novel aminopeptidase N (APN/CD13) inhibitors derived from chloramphenicol amine.

Abstract: Aminopeptidase N (APN) is involved in different physiological and pathological processes of tumor cells, including proliferation, invasion, apoptosis and metastasis. Herein one series of compounds derived from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol have been designed and synthesized. Furthermore, preliminary activity evaluation showed that some compounds elicited moderate inhibitory activity against APN with compounds 10e (IC(50)=6.1##0.5 ##M) possessing the best efficacy, which could be used as the lead compound in the future for anticancer agents research.
(PMID: 21802307)
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
9IC50 data validityIC50 data validityString
* Activity Concentration.

Data Table (Concise)
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Classification
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