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BioAssay: AID 376617

Inhibition of aromatase in human placental microsomes by radiometric method

Natural product drug discovery efforts frequently utilize noncellular screening assays. Fatty acids are commonly found in natural product extracts, and some have been shown to interfere with noncellular assays. Several pure fatty acids were tested using a noncellular aromatase assay, with the unsaturated analogues showing strong inhibitory activity, while the saturated analogues were inactive. more ..
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Active(6)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Active(6)
 
 
Unspecified(1)
 
 
AID: 376617
Data Source: ChEMBL (524646)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Aromatase; AltName: Full=CYPXIX; AltName: Full=Cytochrome P-450AROM; AltName: Full=Cytochrome P450 19A1; AltName: Full=Estrogen synthase
Description ..   
Protein Family: Cytochrome P450
Comment ..   

Gene:CYP19A1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 6
Description:
Title: Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.

Abstract: Natural product drug discovery efforts frequently utilize noncellular screening assays. Fatty acids are commonly found in natural product extracts, and some have been shown to interfere with noncellular assays. Several pure fatty acids were tested using a noncellular aromatase assay, with the unsaturated analogues showing strong inhibitory activity, while the saturated analogues were inactive. Unsaturated fatty acids were further tested against SK-BR-3 hormone-independent human breast cancer cells that overexpress aromatase and were found to be inactive. In natural product screening efforts, especially using plant seeds, it is recommended that extracts active in noncellular bioassays should be dereplicated for the presence of fatty acids prior to bioassay-guided fractionation.
(PMID: 16643058)
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: subcellular 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 valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 binding domainsIC50 binding domainsString

* Activity Concentration.

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