Online parallel fragment screening and rapid hit exploration for nicotinic acetylcholine receptors.

G.E. de Kloe, J. Kool, R. van Elk, J.E. van Muijlwijk-Koezen, A.B. Smit, H. Lingeman, H. Irth, W.M.A. Niessen, I.J.P. de Esch

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

An online bioaffinity analysis system was used to screen our in-house fragment library on two related proteins, Ls- and Ac-AChBP, model proteins for nAChRs, in particular the α7 subtype. An efficient protocol for medium throughput fragment screening, hit validation and affinity ranking after single concentration injections was developed. The screening of the fragment library and the good correlation between online estimated pK
Original languageEnglish
Pages (from-to)590-595
JournalMedChemComm
Volume2
DOIs
Publication statusPublished - 2011

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