JNJ-63533054 induced luciferase activity against zebrafish GPR139 in a concentration-dependent manner. For zebrafish GPR139, the maximal induction of 3.3-fold of vehicle control was achieved at a concentration of 128nM. From the dose-response curve, the half effective maximal concentration (EC50) values of JNJ-63533054 to zebrafish GPR139 was 3.91nM.[1]

JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM). [2]
JNJ-63533054 crosses the rat blood-brain barrier after oral administration and achieves exposure in the micromolar range. JNJ-63533054 administration decreases spontaneous locomotor activity in rats.[2]