Agonist activity at VDR in human SCC25 cells assessed as induction of CYP24 expression at 1 to 10 uM by semiquantitative analysis - BioAssay Summary
Vitamin D receptor (VDR) antagonists have therapeutic potential in treatment of allergic conditions and hypercalcemia driven by granulomatous diseases. We have identified an o-aminoanilide analogue of the hormonal form of vitamin D with a dienyl side chain that functions as a strong VDR antagonist. Modeling studies indicate that antagonism arises from side chain rigidity, when compared to a more flexible saturated analogue, which interferes with H12 folding/alignment. ..more
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(2)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(2)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 527092
Data Source: ChEMBL (674973)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2013-05-13

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=Vitamin D3 receptor; Short=VDR; AltName: Full=1,25-dihydroxyvitamin D3 receptor; AltName: Full=Nuclear receptor subfamily 1 group I member 1
Description ..   
Protein Family: The ligand binding domain of vitamin D receptors, a member of the nuclear receptor superfamily
Comment ..   

Gene:VDR     Related Protein 3D Structures
BioActive Compounds: 2
Description:
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Title: An o-aminoanilide analogue of 1##,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.

Abstract: Vitamin D receptor (VDR) antagonists have therapeutic potential in treatment of allergic conditions and hypercalcemia driven by granulomatous diseases. We have identified an o-aminoanilide analogue of the hormonal form of vitamin D with a dienyl side chain that functions as a strong VDR antagonist. Modeling studies indicate that antagonism arises from side chain rigidity, when compared to a more flexible saturated analogue, which interferes with H12 folding/alignment.
(PMID: 20883026)
Categorized Comment
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ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 64

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

Data Table (Concise)
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Classification
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