Bookmark and Share
BioAssay: AID 590164

Antagonist activity at human CD36-oxLDL binding after 2 hrs by ELISA

By using human scavenger receptor CD36 as the target, twenty-five N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their antagonistic activities for CD36-oxidatively low density lipoprotein (oxLDL) binding. The primary analysis of structure-activity relationship (SAR) indicated a methoxyl at the 7-position and a hydroxyl at the 6- or 8-position could afford more ..
_
   
 Tested Compounds
 Tested Compounds
All(6)
 
 
Unspecified(6)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Unspecified(6)
 
 
 Related BioAssays
 Related BioAssays
AID: 590164
Data Source: ChEMBL (740315)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-08-23

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Platelet glycoprotein 4; AltName: Full=Fatty acid translocase; Short=FAT; AltName: Full=Glycoprotein IIIb; Short=GPIIIB; AltName: Full=Leukocyte differentiation antigen CD36; AltName: Full=PAS IV; AltName: Full=PAS-4; AltName: Full=Platelet collagen receptor; AltName: Full=Platelet glycoprotein IV; Short=GPIV; AltName: Full=Thrombospondin receptor; AltName: CD_antigen=CD36
Description ..   
Protein Family: CD36 family
Comment ..   

Gene:CD36          More BioActivity Data..
Tested Compounds:
Description:
Title: Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists.

Abstract: By using human scavenger receptor CD36 as the target, twenty-five N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their antagonistic activities for CD36-oxidatively low density lipoprotein (oxLDL) binding. The primary analysis of structure-activity relationship (SAR) indicated a methoxyl at the 7-position and a hydroxyl at the 6- or 8-position could afford good activities. Among these analogs, compounds 7e and 7t showed the potential CD36 antagonistic activities with IC(50) values of 0.2 and 0.8 mug/mL, respectively. Furthermore, both of them could effectively inhibit oxLDL uptake in insect Sf9 cells overexpressing human CD36, and thus have been selected for further investigation. We consider N-(2-arylethyl) isoquinoline analogs to be a family of novel CD36 antagonists.
(PMID: 21295889)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50 activity commentIC50 activity commentString
2IC50 standard flagIC50 standard flagInteger
3IC50 qualifierIC50 qualifierString
4IC50 published valueIC50 published valueFloatug ml-1
5IC50 standard valueIC50 standard valueFloatug.mL-1
6IC50 binding domainsIC50 binding domainsString

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
PageFrom: