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Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).
TLDR
By use of parallel chemistry coupled with physicochemical property design, a series of selective κ opioid antagonists have been discovered and 2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan- 1-amine, PF-4455242, which entered phase 1 clinical testing and has demonstrated target engagement in healthy volunteers. Expand