VU0238441

Names

[ Name ]:
VU0238441

[Synonym ]:
VU0238441

Biological Activity

[Description]:

VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

[Target]

EC50: 3.2 μM (M1), 2.8 μM (M2), 2.2 μM (M3), 2.1 μM (M5) and >10 μM (M4)[1]

[In Vitro]

VU0238441 is an analogue of VU0119498[2].

[References]

[1]. Thomas M Bridges, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62.

[2]. Thomas M Bridges, et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₉ClF₃NO₂

[ Molecular Weight ]:
339.69600

[ Exact Mass ]:
339.02700

[ PSA ]:
37.38000

[ LogP ]:
4.15330

Safety Information

[ Hazard Codes ]:
Xn

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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