molecules of the month


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

Chemical structure of the TAK-041 Takeda GPR139 agonist
1 min read

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 deficits in social behavior and cognitive abilities, and GPR139 KO’s demonstrate behavior deficits related to SCZ. Jake Schwarz notes: “While GPCRs are highly druggable, the agonist route is fraught with peril. Full agonism rarely mimics the natural state of a healthy receptor, where the agonist is not constantly present at the receptor. Partial agonists and PAMs have enjoyed much more success.” This first-in-class molecule is a notable example of clinical development of a…

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