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BioAssay: AID 630810

Antagonist activity at FPR1 in whole blood assessed as CD11 level

A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest. ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(2)
 
 
 Related BioAssays
 Related BioAssays
AID: 630810
Data Source: ChEMBL (788258)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
BioActive Compounds: 2
Description:
Title: Discovery of pyrazoles as novel FPR1 antagonists.

Abstract: A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest.
(PMID: 21955939)
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
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
2Kd activity commentKd activity commentString
3Kd standard flagKd standard flagInteger
4Kd qualifierKd qualifierString
5Kd published valueKd published valueFloat
6Kd standard valueKd standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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