Inhibition of CoCl2-induced HIF1alpha expression in mouse 4T1 cells transfected with oxygen-dependent-degradation domain of HIFalpha by luciferase reporter gene assay - BioAssay Summary
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(3)
 
 
Active(2)
 
 
Inactive(2)
 
 
 Tested Substances
 Tested Substances
All(4)
 
 
Active(2)
 
 
Inactive(2)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 425409
Data Source: ChEMBL (576753)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-05-11

Data Table (Complete):           Active    All
Target
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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
BioActive Compounds: 2
Description:
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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
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Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 102395

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4Activity activity commentActivity activity commentString
5Activity standard flagActivity standard flagInteger
6Activity qualifierActivity qualifierString
7Activity published valueActivity published valueFloat
8Activity standard valueActivity standard valueFloat
9IC50 activity commentIC50 activity commentString
10IC50 standard flagIC50 standard flagInteger
11IC50 qualifierIC50 qualifierString
12IC50 published valueIC50 published valueFloatnM
13IC50 standard valueIC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
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Classification
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