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BioAssay: AID 590162

Antagonist activity at human CD36-oxLDL binding at 10 uM 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 ..
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 Tested Compounds
 Tested Compounds
All(26)
 
 
Unspecified(26)
 
 
 Tested Substances
 Tested Substances
All(26)
 
 
Unspecified(26)
 
 
 Related BioAssays
 Related BioAssays
AID: 590162
Data Source: ChEMBL (740313)
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 - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

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