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JNJ 63533054 is a potent and selective GPR139 agonist (EC50 = 16 nM) that is brain and cell penetrant. JNJ 63533054 is selective for GPR139 over a panel of GPCRs, ion channels and transporters, including GPR142 and is orally bioavailable.
[1]. Dvorak CA, et al. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.
[2]. Liu C, et al. GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine. Mol Pharmacol. 2015 Nov;88(5):911-25.
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