Structure-based virtual screening for fragment-like ligands of the G protein-coupled histamine H4 receptor
Author:
Affiliation:
1. Division of Medicinal Chemistry
2. Amsterdam Institute for Molecules, Medicines and Systems (AIMMS)
3. Faculty of Exact Sciences
4. VU University Amsterdam
5. 1081 HV Amsterdam
6. Griffin Discoveries B.V.
7. The Netherlands
Abstract
Structure-based virtual screening using H1R- and β2R-based histamine H4R homology models identified 9 fragments with an affinity ranging from 0.14 to 6.3 μm for H4R.
Publisher
Royal Society of Chemistry (RSC)
Subject
Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2015/MD/C5MD00022J
Reference109 articles.
1. Structural diversity of G protein-coupled receptors and significance for drug discovery
2. En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family
3. The Emerging Role of the Histamine H4 Receptor in Anti-inflammatory Therapy
4. Molecular Determinants of Selective Agonist and Antagonist Binding to the Histamine H4 Receptor
5. Major advances in the development of histamine H4 receptor ligands
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