Publications on Small CXCR3 Antagonists

2-lmino-benzimidazoles. Researchers from Abbott Laboratories found 17 as a HTS hit (IC50 = 3 I-CXCLIO) [80[. Solubility problems led them to replace the 2-acetyl- 

TAK-779. CCR5-hgand TAK-779 (30) has to some extent functioned as a CXCR3-tool as it proved to have moderate affinity for mouse CXCR3 (ICso= 369nM, I-CXCLIO) [85]. However, its poor CXCR3/CCR5 selectivity profile has left TAK-779 only of limited value. 

Antagonists from Natural Sources. Merck performed a screen ( I-CXCLIO) on a library consisting of extracts from microbial, plant and marine sources [86]. A diverse series of hits was found, including sugar-derivatized steroids and dipyridinium salts. 

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