Screening a fragment cocktail library using ultrafiltration

Sayaka Shibata, Zhongsheng Zhang, Konstantin V. Korotkov, Jaclyn Delarosa, Alberto Napuli, Angela M. Kelley, Natasha Mueller, Jennifer Ross, Frank H. Zucker, Frederick S. Buckner, Ethan A. Merritt, Christophe L.M.J. Verlinde, Wesley C. Van Voorhis, Wim G.J. Hol, Erkang Fan

Research output: Contribution to journalArticlepeer-review

8 Scopus citations


Ultrafiltration provides a generic method to discover ligands for protein drug targets with millimolar to micromolar K d, the typical range of fragment-based drug discovery. This method was tailored to a 96-well format, and cocktails of fragment-sized molecules, with molecular masses between 150 and 300 Da, were screened against medical structural genomics target proteins. The validity of the method was confirmed through competitive binding assays in the presence of ligands known to bind the target proteins.

Original languageEnglish
Pages (from-to)1589-1595
Number of pages7
JournalAnalytical and Bioanalytical Chemistry
Issue number5
StatePublished - Sep 2011

Bibliographical note

Funding Information:
We thank Eric T. Larson for his critical review of the manuscript. This work was supported by National Institutes of Health grants P50GM64655 (SGPP), P01AI067921 (MSGPP), and AI34501.


  • Compound library
  • Fragment-based drug discovery
  • Screening
  • Ultrafiltration

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry


Dive into the research topics of 'Screening a fragment cocktail library using ultrafiltration'. Together they form a unique fingerprint.

Cite this