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Description: JNJ-54175446 is a novel, potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively. JNJ-5417544 has suitable physicochemical properties, metabolic stability and an excellent pharmacokinetic profile, good partitioning into the CNS and show robust in vivo target engagement after oral dosing. JNJ-54175446 has been advanced as a candidate to clinical development.
References: J Med Chem. 2017 Jun 8; 60(11):4559-4572
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