AI 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.
Article Abstract
We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, high selectivity, weak hERG activity, and an excellent in vitro and in vivo ADMET profile. INCB8761/PF-4136309 has entered human clinical trials.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018168 | PMC |
| http://dx.doi.org/10.1021/ml200199c | DOI Listing |
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