KLIFS: a structural kinase-ligand interaction database
Kooistra, Albert J, Kanev, Georgi K, van Linden, Oscar P J, Leurs, Rob, de Esch, Iwan J P, de Graaf, Chris
Published in Nucleic acids research (04.01.2016)
Published in Nucleic acids research (04.01.2016)
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Journal Article
Exploring the Effect of Cyclization of Histamine H1 Receptor Antagonists on Ligand Binding Kinetics
Wang, Zhiyong, Bosma, Reggie, Kuhne, Sebastiaan, van den Bor, Jelle, Garabitian, Wrej, Vischer, Henry F, Wijtmans, Maikel, Leurs, Rob, de Esch, Iwan J.P
Published in ACS omega (18.05.2021)
Published in ACS omega (18.05.2021)
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Journal Article
Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain
Akdemir, Atilla, Edink, Ewald, Thompson, Andrew J., Lummis, Sarah C.R., Kooistra, Albert J., de Graaf, Chris, de Esch, Iwan J.P.
Published in Bioorganic & medicinal chemistry (01.10.2012)
Published in Bioorganic & medicinal chemistry (01.10.2012)
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Journal Article
Phenyldihydropyrazolones as Novel Lead Compounds Against Trypanosoma cruzi
Sijm, Maarten, Siciliano de Araújo, Julianna, Kunz, Stefan, Schroeder, Susanne, Edink, Ewald, Orrling, Kristina M, Matheeussen, An, van de Meer, Tiffany, Sadek, Payman, Custers, Hans, Cotillo, Ignacio, Martin, Julio J, Siderius, Marco, Maes, Louis, Brown, David G, de Nazaré Correia Soeiro, Maria, Sterk, GeertJan, de Esch, Iwan J.P, Leurs, Rob
Published in ACS omega (30.04.2019)
Published in ACS omega (30.04.2019)
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Journal Article
A Photoswitchable Agonist for the Histamine H3 Receptor, a Prototypic Family A G‐Protein‐Coupled Receptor
Hauwert, Niels J., Mocking, Tamara A. M., Da Costa Pereira, Daniel, Lion, Ken, Huppelschoten, Yara, Vischer, Henry F., De Esch, Iwan J. P., Wijtmans, Maikel, Leurs, Rob
Published in Angewandte Chemie International Edition (26.03.2019)
Published in Angewandte Chemie International Edition (26.03.2019)
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Journal Article
The histamine H3 receptor: from gene cloning to H3 receptor drugs
Leurs, Rob, Bakker, Remko A, Timmerman, Henk, de Esch, Iwan J P
Published in Nature reviews. Drug discovery (01.02.2005)
Published in Nature reviews. Drug discovery (01.02.2005)
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Journal Article
Photoswitching the Efficacy of a Small‐Molecule Ligand for a Peptidergic GPCR: from Antagonism to Agonism
Gómez‐Santacana, Xavier, de Munnik, Sabrina M., Vijayachandran, Prashanna, Da Costa Pereira, Daniel, Bebelman, Jan Paul M., de Esch, Iwan J. P., Vischer, Henry F., Wijtmans, Maikel, Leurs, Rob
Published in Angewandte Chemie International Edition (03.09.2018)
Published in Angewandte Chemie International Edition (03.09.2018)
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Journal Article
Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation
CORUZZI, Gabriella, ADAMI, Maristella, GUAITA, Elena, DE ESCH, Iwan J. P, LEURS, Rob
Published in European journal of pharmacology (01.06.2007)
Published in European journal of pharmacology (01.06.2007)
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Journal Article
Targeted LC-MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA
Eggink, Mark, Wijtmans, Maikel, Kretschmer, Ansgar, Kool, Jeroen, Lingeman, Henk, de Esch, Iwan J. P, Niessen, Wilfried M. A, Irth, Hubertus
Published in Analytical and bioanalytical chemistry (01.05.2010)
Published in Analytical and bioanalytical chemistry (01.05.2010)
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Journal Article
Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists
Wijtmans, Maikel, Maussang, David, Sirci, Francesco, Scholten, Danny J., Canals, Meritxell, Mujić-Delić, Azra, Chong, Milagros, Chatalic, Kristell L.S., Custers, Hans, Janssen, Elwin, de Graaf, Chris, Smit, Martine J., de Esch, Iwan J.P., Leurs, Rob
Published in European journal of medicinal chemistry (01.05.2012)
Published in European journal of medicinal chemistry (01.05.2012)
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Journal Article
Combinatorial Consensus Scoring for Ligand-Based Virtual Fragment Screening: A Comparative Case Study for Serotonin 5‑HT3A, Histamine H1, and Histamine H4 Receptors
Schultes, Sabine, Kooistra, Albert J, Vischer, Henry F, Nijmeijer, Saskia, Haaksma, Eric E. J, Leurs, Rob, de Esch, Iwan J. P, de Graaf, Chris
Published in Journal of chemical information and modeling (26.05.2015)
Published in Journal of chemical information and modeling (26.05.2015)
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Journal Article
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: Comparison of hERG binding and target residence time with PF-3893787
Andaloussi, Mounir, Lim, Herman D., van der Meer, Tiffany, Sijm, Maarten, Poulie, Chris B.M., de Esch, Iwan J.P., Leurs, Rob, Smits, Rogier A.
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
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Journal Article
Online Fluorescence Enhancement Assay for the Acetylcholine Binding Protein with Parallel Mass Spectrometric Identification
Kool, Jeroen, de Kloe, Gerdien E, Bruyneel, Ben, de Vlieger, Jon S, Retra, Kim, Wijtmans, Maikel, van Elk, Rene, Smit, August B, Leurs, Rob, Lingeman, Henk, de Esch, Iwan J.P, Irth, Hubertus
Published in Journal of medicinal chemistry (24.06.2010)
Published in Journal of medicinal chemistry (24.06.2010)
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Journal Article
Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors
Akdemir, Atilla, Rucktooa, Prakash, Jongejan, Aldo, Elk, Rene van, Bertrand, Sonia, Sixma, Titia K., Bertrand, Daniel, Smit, August B., Leurs, Rob, de Graaf, Chris, de Esch, Iwan J.P.
Published in Bioorganic & medicinal chemistry (15.10.2011)
Published in Bioorganic & medicinal chemistry (15.10.2011)
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Journal Article
Erratum to “ En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family” [Trends Pharmacol. Sci. 32 (4) (2011) 250–257]
Leurs, Rob, Vischer, Henry F, Wijtmans, Maikel, de Esch, Iwan J.P
Published in Trends in pharmacological sciences (Regular ed.) (2012)
Published in Trends in pharmacological sciences (Regular ed.) (2012)
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