Publications by authors named "Lou Storace"
Article Synopsis
- A new series of (S)-3-aminopyrrolidine compounds targeting CCR2 has been discovered.
- Structure-activity relationship studies identified a potent compound, 17 (INCB8761/PF-4136309), with high selectivity and low hERG activity, indicating a favorable safety profile.
- INCB8761/PF-4136309 has advanced to human clinical trials, highlighting its potential as a therapeutic option.
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.
View Article and Find Full Text PDFRational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mCCR2). Modification on 9a led to the discovery of a potent CCR2 antagonist 21 (INCB3344) with IC(50) values of 5.1 nM (hCCR2) and 9.
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