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BioAssay: AID 604305

Inhibition of rabbit 15-LO using linoleic acid by standard colorimetric assay

A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays. ..more
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 Tested Compounds
 Tested Compounds
All(21)
 
 
Active(21)
 
 
 Tested Substances
 Tested Substances
All(21)
 
 
Active(21)
 
 
AID: 604305
Data Source: ChEMBL (754315)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-25

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Arachidonate 15-lipoxygenase; Short=15-LOX; AltName: Full=12/15-lipoxygenase; AltName: Full=Arachidonate 12-lipoxygenase, leukocyte-type; Short=12-LOX; Short=L-12LO; AltName: Full=Arachidonate omega-6 lipoxygenase; AltName: Full=Erythroid cell-specific 15-lipoxygenase
Description ..   
Protein Family: PLAT_LOX
Comment ..   

Gene:ALOX15     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 21
Description:
Title: Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.

Abstract: A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays.
(PMID: 21696952)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloatnM
10IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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