In vitro inhibition of [3H]-LTD4 binding to LTD4 receptor of DMSO differentiated human U937 cell membranes - BioAssay Summary
The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singulair) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists including 2ab (L-733,321) as an optimized candidate. ..more
 _
   
 Tested Compounds
 Tested Compounds
All(12)
 
 
Active(12)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Active(12)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 102799
Data Source: ChEMBL (99993)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2013-04-26

Data Table (Complete):           Active    All
Target
Helptop of page
Sequence: RecName: Full=Cysteinyl leukotriene receptor 1; Short=CysLTR1; AltName: Full=Cysteinyl leukotriene D4 receptor; Short=LTD4 receptor; AltName: Full=G-protein coupled receptor HG55; AltName: Full=HMTMF81
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx
Comment ..   

Gene:CYSLTR1     Related Protein 3D Structures
BioActive Compounds: 12
Description:
Helptop of page
Title: A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

Abstract: The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singulair) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists including 2ab (L-733,321) as an optimized candidate.
(PMID: 9871597)
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: 179

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: