Identification of novel series of human CCR1 antagonists

A hit-to-lead optimization process was carried out on the high throughput screening hit compound 1 resulting in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC50 values of <100 nM in binding and functional assays.

Graphical abstractA hit-to-lead optimization process on the high throughput screening hit compound 1 resulted in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC50 values of <0.01 μM in binding and functional assays.Figure optionsDownload full-size imageDownload as PowerPoint slide