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Coupled enzyme activity and thermal shift screening of the Maybridge Rule of 3 Fragment Library against Trypanosoma brucei choline kinase, a genetically validated drug target Preview this item
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Coupled enzyme activity and thermal shift screening of the Maybridge Rule of 3 Fragment Library against Trypanosoma brucei choline kinase, a genetically validated drug target

Author: Louise L Major; Helen Denton; Terry K Smith
Publisher: Rijeka (HR) : InTech, 2013 Jan 23.
Edition/Format:   Downloadable article : Document   Computer File : EnglishView all editions and formats
Publication:Drug discovery
Summary:
In this study the authors interrogate ~630 compounds of the Maybridge Rule of 3 Fragment Library for compounds that interact with, and inhibit TbCK. The Maybridge Rule of 3 Fragment Library is a small collection of quantifiable diverse [35, 36], pharmacophoric rich, chemical entities. Comparisons between two different screening methods, a coupled enzyme activity assay and differential scanning fluorimetry, has  Read more...
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Details

Genre/Form: Electronic book
Material Type: Document, Internet resource
Document Type: Internet Resource, Article, Computer File
All Authors / Contributors: Louise L Major; Helen Denton; Terry K Smith
ISBN: 9789535109068
OCLC Number: 1030819386
Notes: Chapter 14 of the book: Drug discovery / edited by Hany A. El-Shemy. Rijeka, Croatia : InTech, 2013.
Description: 1 online resource : illustrations
Other Titles: Drug discovery.
Responsibility: Louise L. Major, Helen Denton, and Terry K. Smith.

Abstract:

In this study the authors interrogate ~630 compounds of the Maybridge Rule of 3 Fragment Library for compounds that interact with, and inhibit TbCK. The Maybridge Rule of 3 Fragment Library is a small collection of quantifiable diverse [35, 36], pharmacophoric rich, chemical entities. Comparisons between two different screening methods, a coupled enzyme activity assay and differential scanning fluorimetry, has allowed identification of compounds that interact and inhibit the T. brucei choline kinase, several of which possess selective trypanocidal activity.

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