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BioAssay: AID 594626

Reversible inhibition of FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilisation by FLIPR assay

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)
 
 
AID: 594626
Data Source: ChEMBL (744777)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-05-24

Data Table ( Complete ):           View Active Data    View All Data
Target
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     More BioActivity Data..
BioActive Compounds: 2
Description:
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)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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