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BioAssay: AID 620272

Inhibition of 5-Lipoxygenase in arachidonic acid-stimulated human neutrophils assessed as residual activity at 10 uM after 15 mins by HPLC analysis in presence of A23187

We recently presented that compounds 4a-b moderately inhibited leukotriene (LT) formation in human neutrophils. For structural derivatization of 4a-b, novel thirty-six title compounds were synthesized and led to more potent inhibition of LT biosynthesis in activated human neutrophils exemplified by compounds 15, 27-30, 32-37, 41, 42 with IC(50) values in the range of 1.6-3.5 muM. Moreover, more ..
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 Tested Compounds
 Tested Compounds
All(36)
 
 
Unspecified(36)
 
 
 Tested Substances
 Tested Substances
All(36)
 
 
Unspecified(36)
 
 
 Related BioAssays
 Related BioAssays
AID: 620272
Data Source: ChEMBL (770283)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-26

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Arachidonate 5-lipoxygenase; Short=5-LO; Short=5-lipoxygenase
Description ..   
Protein Family: Lipoxygenase
Comment ..   

Gene:ALOX5     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Pyrazol-3-propanoic acid derivatives as novel inhibitors of leukotriene biosynthesis in human neutrophils.

Abstract: We recently presented that compounds 4a-b moderately inhibited leukotriene (LT) formation in human neutrophils. For structural derivatization of 4a-b, novel thirty-six title compounds were synthesized and led to more potent inhibition of LT biosynthesis in activated human neutrophils exemplified by compounds 15, 27-30, 32-37, 41, 42 with IC(50) values in the range of 1.6-3.5 muM. Moreover, compounds 32, 35, 42, 43 and 44 showed a substantial inhibition of platelet COX-1 activity with IC(50) of 2.5, 0.041, 0.3, 0.9 and 0.014 muM, respectively, leading up to dual acting inhibitors. On the basis of their high potency in cellular environment, these straightforward pyrazole-3-propanoic acid derivatives may possess potential in the design of more potent compounds for intervention with inflammatory and allergic diseases.
(PMID: 21868137)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Protein Target Class: enzyme reductase

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)
Data Table ( Complete ):     View All Data
Classification
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