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BioAssay: AID 426478

Cytotoxicity against mouse L1.2 cells assessed as cell viability by trypan blue dye exclusion assay

We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the fine role of the propionic/acetic chain in the modulation of CXCL8 receptors. ..more
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 Tested Compounds
 Tested Compounds
All(27)
 
 
Unspecified(27)
 
 
 Tested Substances
 Tested Substances
All(27)
 
 
Unspecified(27)
 
 
 Related BioAssays
 Related BioAssays
AID: 426478
Data Source: ChEMBL (577822)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-07-06

Data Table ( Complete ):           All
Tested Compounds:
Description:
Title: Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.

Abstract: We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the fine role of the propionic/acetic chain in the modulation of CXCL8 receptors.
(PMID: 19560921)
Comment
Putative Target:

ChEMBL Target ID: 100521
Target Type: CELL-LINE
Cell Line: L1.2
Tissue: Pre-B cells
Pref Name: L1.2
Organism: Mus musculus
Tax ID: 10090
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment
ChEMBL Assay Type: ADMET

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Assay Cell Type: L1.2

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
PageFrom: