Výsledky vyhledávání - "Jerri L. Rook"

Akademický článek

Discovery of 'Molecular Switches' within a Series of mGlu5 Allosteric Ligands Driven by a 'Magic Methyl' Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype

Autor: Lisa Barbaro, Alice L. Rodriguez, Ashlyn N. Blevins, Jonathan W. Dickerson, Natasha Billard, Olivier Boutaud, Jerri L. Rook, Colleen M. Niswender, P.Jeffrey Conn, Darren W. Engers, Craig W. Lindsley

Publikováno v: ACS Bio & Med Chem Au, Vol 1, Iss 1, Pp 21-30 (2021)

Externí odkaz: https://doaj.org/article/a1962d9086d84ecabe40eff8d58cb02f

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Discovery of 'Molecular Switches' within a Series of mGlu5 Allosteric Ligands Driven by a 'Magic Methyl' Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype

Autor: Darren W. Engers, Natasha Billard, Colleen M. Niswender, Ashlyn N. Blevins, Olivier Boutaud, Jonathan W. Dickerson, P. Jeffrey Conn, Jerri L. Rook, Craig W. Lindsley, Alice L. Rodriguez, Lisa Barbaro

Publikováno v: ACS Bio & Med Chem Au, Vol 1, Iss 1, Pp 21-30 (2021)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c6207100701021f062c871e381bbd20f
https://doaj.org/article/a1962d9086d84ecabe40eff8d58cb02f

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Discovery and optimization of a novel CNS penetrant series of mGlu

Autor: Caitlin N, Kent, Mark G, Fulton, Kaylee J, Stillwell, Jonathan W, Dickerson, Matthew T, Loch, Alice L, Rodriguez, Anna L, Blobaum, Olivier, Boutaud, Jerri L, Rook, Colleen M, Niswender, P Jeffrey, Conn, Craig W, Lindsley

Publikováno v: Bioorganicmedicinal chemistry letters. 37

A high throughput screen (HTS) identified a novel, but weak (EC

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::aa0e4acb766ebacc10e8996ddcf9fb14
https://pubmed.ncbi.nlm.nih.gov/33556572

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Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model

Autor: Kaylee J. Stillwell, Jonathan W. Dickerson, Matthew T. Loch, Craig W. Lindsley, Mark G. Fulton, Olivier Boutaud, P. Jeffrey Conn, Colleen M. Niswender, Caitlin N. Kent, Alice L. Rodriguez, Jerri L. Rook, Anna L. Blobaum

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 37:127838

A high throughput screen (HTS) identified a novel, but weak (EC50 = 6.2 μM, 97% Glu Max) mGlu4 PAM chemotype based on a 1,4-thiazepane core, VU0544412. Reaction development and chemical optimization delivered a potent mGlu4 PAM VU6022296 (EC50 = 32.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8982a8ca4fb9fbb1b11c0095cf87e8fb
https://doi.org/10.1016/j.bmcl.2021.127838

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