The Takeda GPR139 agonist, TAK-041 , is a CNS-penetrant GPCR agonist being explored for schizophrenia symptoms and is an interesting example of a triazinone-containing clinical candidate. GPR139 is an orphan GPCR that’s highly expressed in the human habenula, which plays a major role in avoidance behavior. Lesions in the habenula cause [...]
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Dec. 16, 2021
TAK-041: a GPR139 Agonist
TAK-041
GPR139 GPCR agonist oral (40-160 mg QD) Ph. II for schizophrenia 625k-cmpd cell-based screen (21 nM hit) + opt Journal of Medicinal Chemistry Takeda, San Diego, US
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