Literature DB >> 10784141

A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates.

C D Bevan1, R S Lloyd.   

Abstract

The determination of aqueous solubility in a high-throughput screening environment is invaluable in the selection of the most promising potential drug candidates. We describe a fast method based on laser nephelometry that can determine the solubility of potential drug candidates (usually from combinatorial chemistry) supplied as dimethyl sulfoxide (DMSO) solutions in 96-well plates. In the sample, the percent DMSO is kept constant allowing direct comparison of results. The nephelometric method has been shown to produce results equivalent to those produced by an HPLC method and to be largely unaffected by colored solutions.

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Year:  2000        PMID： 10784141     DOI： 10.1021/ac9912247

Source DB:  PubMed          Journal:  Anal Chem        ISSN： 0003-2700            Impact factor:   6.986


  42 in total

1.  Solubility at the molecular level: development of a critical aggregation concentration (CAC) assay for estimating compound monomer solubility.

Authors:  Jie Wang; Edmund Matayoshi
Journal:  Pharm Res       Date:  2012-03-16       Impact factor: 4.200

2.  Progress in antischistosomal N,N'-diaryl urea SAR.

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Journal:  Bioorg Med Chem Lett       Date:  2017-12-29       Impact factor: 2.823

3.  Discovery pharmaceutics--challenges and opportunities.

Authors:  Xue-Qing Chen; Melissa D Antman; Christoph Gesenberg; Olafur S Gudmundsson
Journal:  AAPS J       Date:  2006-06-02       Impact factor: 4.009

4.  High-throughput identification of inhibitors of human mitochondrial peptide deformylase.

Authors:  Christophe Antczak; David Shum; Sindy Escobar; Bhramdeo Bassit; Earl Kim; Venkatraman E Seshan; Nian Wu; Guangli Yang; Ouathek Ouerfelli; Yue-Ming Li; David A Scheinberg; Hakim Djaballah
Journal:  J Biomol Screen       Date:  2007-04-13

5.  Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.

Authors:  Georgina A Holloway; William N Charman; Alan H Fairlamb; Reto Brun; Marcel Kaiser; Edmund Kostewicz; Patrizia M Novello; John P Parisot; John Richardson; Ian P Street; Keith G Watson; Jonathan B Baell
Journal:  Antimicrob Agents Chemother       Date:  2009-04-13       Impact factor: 5.191

6.  Monitoring of HTS compound library quality via a high-resolution image acquisition and processing instrument.

Authors:  Pierre Baillargeon; Louis Scampavia; Ross Einsteder; Peter Hodder
Journal:  J Lab Autom       Date:  2011-05-16

7.  Interpreting physicochemical experimental data sets.

Authors:  Nicola Colclough; Mark C Wenlock
Journal:  J Comput Aided Mol Des       Date:  2015-06-09       Impact factor: 3.686

8.  A new chemotype with promise against Trypanosoma cruzi.

Authors:  Xiaofang Wang; Monica Cal; Marcel Kaiser; Frederick S Buckner; Galina I Lepesheva; Austin G Sanford; Alexander I Wallick; Paul H Davis; Jonathan L Vennerstrom
Journal:  Bioorg Med Chem Lett       Date:  2019-10-31       Impact factor: 2.823

9.  Development of second generation EP2 antagonists with high selectivity.

Authors:  Thota Ganesh; Jianxiong Jiang; Ray Dingledine
Journal:  Eur J Med Chem       Date:  2014-06-03       Impact factor: 6.514

10.  Determination of drug-like properties of a novel antileishmanial compound: In vitro absorption, distribution, metabolism, and excretion studies.

Authors:  Susanta Kumar Mondal; Nirup B Mondal; Sukdeb Banerjee; Upal Kanti Mazumder
Journal:  Indian J Pharmacol       Date:  2009-08       Impact factor: 1.200
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