473719-41-4Relevant academic research and scientific papers
Synthesis and Application of the First Radioligand Targeting the Allosteric Binding Pocket of Chemokine Receptor CXCR3
Bernat, Viachaslau,Heinrich, Markus R.,Baumeister, Paul,Buschauer, Armin,Tschammer, Nuska
experimental part, p. 1481 - 1489 (2012/10/08)
Strategies for the identification of allosteric modulators of chemokine receptors largely rely on various cell-based functional assays. Radioligand binding assays are typically not available for allosteric binding sites. We synthesized, purified, and appl
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3
Johnson, Michael,Li, An-Rong,Liu, Jiwen,Fu, Zice,Zhu, Liusheng,Miao, Shichang,Wang, Xuemei,Xu, Qingge,Huang, Alan,Marcus, Andrew,Xu, Feng,Ebsworth, Karen,Sablan, Emmanuel,Danao, Jay,Kumer, Jeff,Dairaghi, Dan,Lawrence, Chris,Sullivan, Tim,Tonn, George,Schall, Thomas,Collins, Tassie,Medina, Julio
, p. 3339 - 3343 (2008/02/11)
A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a 125I-IP10 displacement assay and in in vitro cell migration assays to IP10, IT
Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists
Storelli, Stefania,Verzijl, Dennis,Al-Badie, Jawad,Elders, Niels,Bosch, Leontien,Timmerman, Henk,Smit, Martine J.,De Esch, Iwan J. P.,Leurs, Rob
, p. 281 - 291 (2008/02/10)
CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-pheny
