Leveraging fragment-based drug discovery to advance 3D scaffolds into potent ligands: application to the histamine H 1 receptor

RSC Medicinal Chemistry 2026 Open access

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Authors: Tom Dekker, Oscar P. J. van Linden, Herman D. Lim, Mabel E. Dekker, Henry F. Vischer, Rob Leurs, Tiffany van der Meer, Maurice C. M. L. Buzink, David J. Cole Hamilton, Barbara A. Zarzycka, Elwin Janssen, Maikel Wijtmans
+1 more Iwan J. P. de Esch
DOI: 10.1039/d5md01081k
Cited by: 0
References: 44

Abstract

Fragment-based drug discovery enables translation of novel (3D) chemistries into biologically relevant hit matter, as demonstrated by the identification and optimization of a cyclobutane-based 3D fragment into a potent histamine H 1 receptor ligand.

Fields of Study & Subjects

Computational Drug Discovery Methods Receptor Mechanisms and Signaling Chemical Synthesis and Analysis

Publication details

Journal / source
RSC Medicinal Chemistry
Volume
17
Issue
3
Pages
1483–1492
Publication date
1 January 2026
Language
EN