Transactivation of human VDR transfected in african green monkey COS7 cells after 24 hrs by luciferase reporter gene assay - BioAssay Summary
We designed by docking and synthesized two novel analogues of 1##,25-dihydroxyvitamin D(3) hydroxymethylated at C-26 (2 and 3). The syntheses were carried out by the convergent Wittig-Horner approach via epoxide 12a as a common key intermediate. The antiproliferative and transactivation potency of the compounds was evaluated in colon and breast cancer cell lines. The analogues showed a similar but reduced activity compared to 1,25(OH)(2)D(3). Analogue 3 was more potent than analogue 2, and in some assays it exhibited potency similar to that of the natural ligand. ..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)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 602057
Data Source: ChEMBL (752208)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2013-05-15

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 Compound: 1
Description:
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Title: Synthesis and biological evaluation of 1##,25-dihydroxyvitamin D(3) analogues hydroxymethylated at C-26.

Abstract: We designed by docking and synthesized two novel analogues of 1##,25-dihydroxyvitamin D(3) hydroxymethylated at C-26 (2 and 3). The syntheses were carried out by the convergent Wittig-Horner approach via epoxide 12a as a common key intermediate. The antiproliferative and transactivation potency of the compounds was evaluated in colon and breast cancer cell lines. The analogues showed a similar but reduced activity compared to 1,25(OH)(2)D(3). Analogue 3 was more potent than analogue 2, and in some assays it exhibited potency similar to that of the natural ligand.
(PMID: 21524075)
Categorized Comment
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ChEMBL Assay Type: Binding

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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