Optimization of M(4) positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

This letter describes the further chemical optimization of the 5-amino-thieno[2,3-c]pyridazine series (VU0467154/VU0467485) of M(4) positive allosteric modulators (PAMs), developed via iterative parallel synthesis, culminating in the discovery of the non-human primate (NHP) in vivo tool compound, VU...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Melancon, Bruce J., Wood, Michael R., Noetzel, Meredith J., Nance, Kellie D., Engelberg, Eileen M., Han, Changho, Lamsal, Atin, Chang, Sichen, Cho, Hyekyung P., Byers, Frank W., Bubser, Michael, Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Engers, Darren W., Wu, Dedong, Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5508548/
https://ncbi.nlm.nih.gov/pubmed/28442253
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.04.043
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