Inhibition of human recombinant CYP24A1 expressed in chinese hamster V79 cells using [3H-1-beta]calcitriol after 60 mins by scintillation counting - BioAssay Summary
A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 microM compared with the standard ketoconazole IC50 0.52 microM, with the styryl derivative (11c) displaying enhanced activity (IC50=0.3 microM) compared with the standard, providing a useful preliminary lead for drug development. ..more
 _
   
 Tested Compounds
 Tested Compounds
All(9)
 
 
Active(8)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Active(8)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 492342
Data Source: ChEMBL (642749)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-12-02
Modify Date: 2013-05-12

Data Table (Complete):           Active    All
Target
Helptop of page
Sequence: RecName: Full=1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial; Short=24-OHase; Short=Vitamin D(3) 24-hydroxylase; AltName: Full=Cytochrome P450 24A1; AltName: Full=Cytochrome P450-CC24; Flags: Precursor
Description ..   
Protein Family: Cytochrome P450
Comment ..   

Gene:CYP24A1     Related Protein 3D Structures
BioActive Compounds: 8
Description:
Helptop of page
Title: Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides.

Abstract: A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 microM compared with the standard ketoconazole IC50 0.52 microM, with the styryl derivative (11c) displaying enhanced activity (IC50=0.3 microM) compared with the standard, providing a useful preliminary lead for drug development.
(PMID: 20594862)
Comment
Helptop of page
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Helptop of page
ChEMBL Assay Type: ADMET

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 100474

ChEMBL target type: Target is a single protein chain

Result Definitions
Helptop of page
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatnM
6IC50 standard valueIC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
Helptop of page
Classification
PageFrom: