Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear leukocyte pretreated for 15 mins measured after 4 hrs by cell migration assay - BioAssay Summary
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
 _
   
 Tested Compounds
 Tested Compounds
All(27)
 
 
Active(19)
 
 
Unspecified(8)
 
 
 Tested Substances
 Tested Substances
All(27)
 
 
Active(19)
 
 
Unspecified(8)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 426392
Data Source: ChEMBL (577736)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-05-11

Data Table (Complete):           Active    All
Target
Helptop of page
Sequence: RecName: Full=Interleukin-8; Short=IL-8; AltName: Full=C-X-C motif chemokine 8; AltName: Full=Emoctakin; AltName: Full=Granulocyte chemotactic protein 1; Short=GCP-1; AltName: Full=Monocyte-derived neutrophil chemotactic factor; Short=MDNCF; AltName: Full=Monocyte-derived neutrophil-activating peptide; Short=MONAP; AltName: Full=Neutrophil-activating protein 1; Short=NAP-1; AltName: Full=Protein 3-10C; AltName: Full=T-cell chemotactic factor; Contains: RecName: Full=MDNCF-a; AltName: Full=GCP/IL-8 protein IV; AltName: Full=IL8/NAP1 form I; Contains: RecName: Full=Interleukin-8; AltName: Full=(Ala-IL-8)77; AltName: Full=GCP/IL-8 protein II; AltName: Full=IL-8(1-77); AltName: Full=IL8/NAP1 form II; AltName: Full=MDNCF-b; Contains: RecName: Full=IL-8(5-77); Contains: RecName: Full=IL-8(6-77); AltName: Full=(Ser-IL-8)72; AltName: Full=GCP/IL-8 protein I; AltName: Full=IL8/NAP1 form III; AltName: Full=Lymphocyte-derived neutrophil-activating factor; Short=LYNAP; AltName: Full=MDNCF-c; AltName: Full=Neutrophil-activating factor; Short=NAF; Contains: RecName: Full=IL-8(7-77); AltName: Full=GCP/IL-8 protein V; AltName: Full=IL8/NAP1 form IV; Contains: RecName: Full=IL-8(8-77); AltName: Full=GCP/IL-8 protein VI; AltName: Full=IL8/NAP1 form V; Contains: RecName: Full=IL-8(9-77); AltName: Full=GCP/IL-8 protein III; AltName: Full=IL8/NAP1 form VI; Flags: Precursor
Description ..   
Protein Family: Chemokine_CXC
Comment ..   

Gene:IL8     Related Protein 3D Structures
BioActive Compounds: 19
Description:
Helptop of page
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
Helptop of page
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Helptop of page
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 10040

ChEMBL target type: Target is a single protein chain

Result Definitions
Helptop of page
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4IC50 activity commentIC50 activity commentString
5IC50 standard flagIC50 standard flagInteger
6IC50 qualifierIC50 qualifierString
7IC50 published valueIC50 published valueFloatnM
8IC50 standard valueIC50 standard valueFloatnM
9IC50 binding domainsIC50 binding domainsString
* Activity Concentration.

Data Table (Concise)
Helptop of page
Classification
PageFrom: