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BioAssay: AID 594625

Antagonist activity at FPR1

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(4)
 
 
Active(4)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Active(5)
 
 
 Related BioAssays
 Related BioAssays
AID: 594625
Data Source: ChEMBL (744776)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
BioActive Compounds: 4
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.

Putative Target:

ChEMBL Target ID: 13010
Target Type: SINGLE PROTEIN
Pref Name: Formyl peptide receptor 1
Synonyms: fMet-Leu-Phe receptor;fMLP receptor;FPR;N-formyl peptide receptor;N-formylpeptide chemoattractant receptor;
Gene Name: FPR1;
Protein Accession: P21462;
Protein GI: 288558848;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: membrane receptor 7tm1 peptide n-formyl methionyl peptide receptor n-formyl methionyl peptide receptor
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

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 valueFloat
6IC50 standard valueIC50 standard valueFloatnM
7Ki activity commentKi activity commentString
8Ki standard flagKi standard flagInteger
9Ki qualifierKi qualifierString
10Ki published valueKi published valueFloat
11Ki standard valueKi standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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