de Esch IJP - Search Results

1

Fragment-to-Lead Medicinal Chemistry Publications in 2021.

Walsh L, Erlanson DA, de Esch IJP, Jahnke W, Woodhead A, Wren E. Walsh L, et al. Among authors: de esch ijp. J Med Chem. 2023 Jan 26;66(2):1137-1156. doi: 10.1021/acs.jmedchem.2c01827. Epub 2023 Jan 9. J Med Chem. 2023. PMID: 36622056 Review.

2

Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.

Hulshof JW, Casarosa P, Menge WM, Kuusisto LM, van der Goot H, Smit MJ, de Esch IJ, Leurs R. Hulshof JW, et al. J Med Chem. 2005 Oct 6;48(20):6461-71. doi: 10.1021/jm050418d. J Med Chem. 2005. PMID: 16190772

3

A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.

Govoni M, Lim HD, El-Atmioui D, Menge WM, Timmerman H, Bakker RA, Leurs R, De Esch IJ. Govoni M, et al. J Med Chem. 2006 Apr 20;49(8):2549-57. doi: 10.1021/jm0504353. J Med Chem. 2006. PMID: 16610798

4

The emerging role of the histamine H4 receptor in anti-inflammatory therapy.

Lim HD, Smits RA, Leurs R, De Esch IJ. Lim HD, et al. Curr Top Med Chem. 2006;6(13):1365-73. doi: 10.2174/15680266106061365. Curr Top Med Chem. 2006. PMID: 16918455 Review.

5

Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.

Smits RA, Lim HD, Hanzer A, Zuiderveld OP, Guaita E, Adami M, Coruzzi G, Leurs R, de Esch IJ. Smits RA, et al. J Med Chem. 2008 Apr 24;51(8):2457-67. doi: 10.1021/jm7014217. Epub 2008 Mar 22. J Med Chem. 2008. PMID: 18357976

6

Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.

Smits RA, de Esch IJ, Zuiderveld OP, Broeker J, Sansuk K, Guaita E, Coruzzi G, Adami M, Haaksma E, Leurs R. Smits RA, et al. J Med Chem. 2008 Dec 25;51(24):7855-65. doi: 10.1021/jm800876b. J Med Chem. 2008. PMID: 19053770

7

Transforming fragments into candidates: small becomes big in medicinal chemistry.

de Kloe GE, Bailey D, Leurs R, de Esch IJ. de Kloe GE, et al. Drug Discov Today. 2009 Jul;14(13-14):630-46. doi: 10.1016/j.drudis.2009.03.009. Epub 2009 Mar 31. Drug Discov Today. 2009. PMID: 19443265 Review.

8

Online fluorescence enhancement assay for the acetylcholine binding protein with parallel mass spectrometric identification.

Kool J, de Kloe GE, Bruyneel B, de Vlieger JS, Retra K, Wijtmans M, van Elk R, Smit AB, Leurs R, Lingeman H, de Esch IJ, Irth H. Kool J, et al. J Med Chem. 2010 Jun 24;53(12):4720-30. doi: 10.1021/jm100230k. J Med Chem. 2010. PMID: 20518527

9

Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands.

de Kloe GE, Retra K, Geitmann M, Källblad P, Nahar T, van Elk R, Smit AB, van Muijlwijk-Koezen JE, Leurs R, Irth H, Danielson UH, de Esch IJ. de Kloe GE, et al. J Med Chem. 2010 Oct 14;53(19):7192-201. doi: 10.1021/jm100834y. J Med Chem. 2010. PMID: 20828128

10

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.

Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ. Verheij MH, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5460-4. doi: 10.1016/j.bmcl.2011.06.123. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21782429 Free PMC article.

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