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BioAssay: AID 683124

Inhibition of recombinant human 15-lipoxygenase by MBTH-DMAB method

All of the mono isopentenyloxy, -geranyloxy and -farnesyloxy derivatives of coumarin were synthesized and their inhibitory potency against soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (HLO-1) were determined. Amongst the synthetic analogs, 5-farnesyloxycoumarin showed the most potent inhibitory activity against SLO (IC(50) = 0.8 I(1/4)M) while 6-farnesyloxycoumarin was the strongest more ..
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 Tested Compounds
 Tested Compounds
All(13)
 
 
Active(10)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(13)
 
 
Active(10)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 683124
Data Source: ChEMBL (840271)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Arachidonate 15-lipoxygenase; Short=15-LOX; Short=15-LOX-1; AltName: Full=12/15-lipoxygenase; AltName: Full=Arachidonate 12-lipoxygenase, leukocyte-type; Short=12-LOX; AltName: Full=Arachidonate omega-6 lipoxygenase
Description ..   
Protein Family: Lipoxygenase
Comment ..   

Gene:ALOX15     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 10
Description:
Title: Synthesis and SAR studies of mono O-prenylated coumarins as potent 15-lipoxygenase inhibitors.

Abstract: All of the mono isopentenyloxy, -geranyloxy and -farnesyloxy derivatives of coumarin were synthesized and their inhibitory potency against soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (HLO-1) were determined. Amongst the synthetic analogs, 5-farnesyloxycoumarin showed the most potent inhibitory activity against SLO (IC(50) = 0.8 I(1/4)M) while 6-farnesyloxycoumarin was the strongest HLO-1 inhibitor (IC(50) = 1.3 I(1/4)M). The IC(50) variations of the farnesyl derivatives for HLO-1 (1.3 to #75 I(1/4)M) were much higher than that observed for SLO (0.8-5.8 I(1/4)M). SAR studies showed that hydrogen bonding, CH/I
(PMID: 23047230)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 12054

ChEMBL Target Type: Target is a single protein chain

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface 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 valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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