Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay - BioAssay Summary
The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target. ..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: 594622
Data Source: ChEMBL (744773)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2013-05-15

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=fMet-Leu-Phe receptor; Short=fMLP receptor; AltName: Full=N-formyl peptide receptor; Short=FPR; AltName: Full=N-formylpeptide chemoattractant receptor
Description ..   
Comment ..   

Gene:FPR1     Conserved Domain     Related Protein 3D Structures
BioActive Compounds: 2
Description:
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Title: Discovery of small molecule human FPR1 receptor antagonists.

Abstract: The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target.
(PMID: 21486695)
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: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 13010

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
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatnM
6IC50 standard valueIC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
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Classification
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