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Sep. 18, 2021

CVN424: A CNS Penetrant GPR6 GPCR Inverse Agonist


CNS pen. GPR6 GPCR inverse agonist oral QD Ph. II candidate for Parkinson's from 360k cmpd cell-based HTS + opt. J. Pharmacol. Exp. Ther., Apr. 1, 2021 Cerevance / Takeda California, San Diego, US

Drug Hunter Team

The Cerevance/Takeda GPR6 inverse agonist (CVN424) is an oral, once-daily clinical candidate in Ph. II for Parkinson’s disease after completing a Ph. I in healthy volunteers. Its >40 µM starting point was discovered through a 360k compound cell-based HTS targeting human GPR6 (an orphan GPCR). The molecule CVN424 is interesting because it is [...]



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