Antagonist activity at CXCR2 in human neutrophils assessed as inhibition of GROalpha-stimulated intracellular calcium mobilization at 50 uM by FLIPR 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)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Unspecified(2)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 594616
Data Source: ChEMBL (744767)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2013-05-15

Data Table (Complete):           All
Target
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Sequence: RecName: Full=C-X-C chemokine receptor type 2; Short=CXC-R2; Short=CXCR-2; AltName: Full=CDw128b; AltName: Full=GRO/MGSA receptor; AltName: Full=High affinity interleukin-8 receptor B; Short=IL-8R B; AltName: Full=IL-8 receptor type 2; AltName: CD_antigen=CD182
Description ..   
Comment ..   

Gene:CXCR2     Conserved Domain     Related Protein 3D Structures
Tested Compounds:
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)
Categorized Comment
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ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 10773

ChEMBL target type: Target is a single protein chain

Result Definitions
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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)
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Classification
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