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BioAssay: AID 594572

Agonist activity at FPR1 in human neutrophils assessed as increase in calcium mobilization 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(6)
 
 
Active(1)
 
 
Unspecified(5)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Active(1)
 
 
Unspecified(5)
 
 
 Related BioAssays
 Related BioAssays
AID: 594572
Data Source: ChEMBL (744723)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
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          More BioActivity Data..
BioActive Compound: 1
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)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
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
1EC50*EC50 PubChem standard valueFloatμM
2EC50 activity commentEC50 activity commentString
3EC50 standard flagEC50 standard flagInteger
4EC50 qualifierEC50 qualifierString
5EC50 published valueEC50 published valueFloat
6EC50 standard valueEC50 standard valueFloatnM
7EC50 binding domainsEC50 binding domainsString
8Inhibition activity commentInhibition activity commentString
9Inhibition standard flagInhibition standard flagInteger
10Inhibition qualifierInhibition qualifierString
11Inhibition published valueInhibition published valueFloat%
12Inhibition standard valueInhibition standard valueFloat%
13Inhibition binding domainsInhibition binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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