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Synthesis and application of the first radioligand targeting the allosteric binding pocket of chemokine receptor CXCR3

Bernat, Viachaslau ; Heinrich, Markus ; Baumeister, Paul ; Buschauer, Armin ; Tschammer, Nuska



Abstract

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 applied the first tritium-labeled allosteric modulator of thehuman chemokine receptor CXCR3 (RAMX3, ...

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