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BioAssay: AID 425409

Inhibition of CoCl2-induced HIF1alpha expression in mouse 4T1 cells transfected with oxygen-dependent-degradation domain of HIFalpha by luciferase reporter gene assay

We have shown that manassantin A downregulated the HIF-1alpha expression and inhibited the secretion of VEGF. We have also demonstrated that the 2,3-cis-3,4-trans-4,5-cis-configuration of the tetrahydrofuran is critical to the HIF-1 inhibition of manassantin A. ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Active(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(1)
 
 
Inactive(1)
 
 
AID: 425409
Data Source: ChEMBL (576753)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Hypoxia-inducible factor 1-alpha; Short=HIF-1-alpha; Short=HIF1-alpha; AltName: Full=ARNT-interacting protein
Description ..   
Protein Family: HIF-1 alpha C terminal transactivation domain
Comment ..   

Gene:HIF1A     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations.

Abstract: We have shown that manassantin A downregulated the HIF-1alpha expression and inhibited the secretion of VEGF. We have also demonstrated that the 2,3-cis-3,4-trans-4,5-cis-configuration of the tetrahydrofuran is critical to the HIF-1 inhibition of manassantin A.
(PMID: 19423348)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: 4T1
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
6Activity activity commentActivity activity commentString
7Activity standard flagActivity standard flagInteger
8Activity qualifierActivity qualifierString
9Activity published valueActivity published valueFloat
10Activity standard valueActivity standard valueFloat
11IC50 activity commentIC50 activity commentString
12IC50 standard flagIC50 standard flagInteger
13IC50 qualifierIC50 qualifierString
14IC50 published valueIC50 published valueFloatnM
15IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

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