JNJ-46281222

Names

[ Name ]:
JNJ-46281222

Biological Activity

[Description]:

JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71)[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

[Target]

mGluR2:1.7 nM (Kd)

[In Vitro]

JNJ‐4628122 binds to the selected mGlu2 receptor mutants is significantly decreased by approximately 10‐fold compared with WT, in transfected mGlu2 WT and mutant receptors in CHO‐K1 cells, mutations F643A and N735D are selected[1]. Western Blot Analysis[1] Cell Line: CHO‐K1 cells Concentration: Incubation Time: Result: Showed a decreased expression of mGlu2 receptor in mutant cells.

[References]

[1]. Doornbos ML,et al. Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.Br J Pharmacol. 2016 Feb;173(3):588-600.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₅F₃N₄

[ Molecular Weight ]:
414.47

Related Compounds

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