Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay - BioAssay Summary
Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with more robust DMPK profiles. These were subsequently improved to generate analogues with attractive overall profiles. ..more
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 Tested Compounds
 Tested Compounds
All(20)
 
 
Active(20)
 
 
 Tested Substances
 Tested Substances
All(20)
 
 
Active(20)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 638993
Data Source: ChEMBL (796441)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
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: 20
Description:
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Title: Lead optimisation of pyrazoles as novel FPR1 antagonists.

Abstract: Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with more robust DMPK profiles. These were subsequently improved to generate analogues with attractive overall profiles.
(PMID: 22094028)
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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