8 research outputs found
Two Messages from the President of the United States Communicating Additional Correspondence in Relation to the Adjustment of the Northeastern Boundary, and the Occupation of the Disputed Territory
Correspondence authored by President Van Buren, American Secretary of State, John Forsyth, Maine Governor, John Fairfield, British Envoy Henry S. Fox, and others regarding the occupation and movement of British soldiers in the disputed territory along the northeastern boundary of the State of Maine between Maine and modern-day New Brunswick, Canada. The border issue was resolved on August 9, 1842 with the Webster-Ashburton Treaty.https://digitalcommons.library.umaine.edu/mainebicentennial/1051/thumbnail.jp
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu<sub>5</sub> Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)
Fragment
screening of a thermostabilized mGlu<sub>5</sub> receptor
using a high-concentration radioligand binding assay enabled the identification
of moderate affinity, high ligand efficiency (LE) pyrimidine hit <b>5</b>. Subsequent optimization using structure-based drug discovery
methods led to the selection of <b>25</b>, HTL14242, as an advanced
lead compound for further development. Structures of the stabilized
mGlu<sub>5</sub> receptor complexed with <b>25</b> and another
molecule in the series, <b>14</b>, were determined at resolutions
of 2.6 and 3.1 Ă
, respectively
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu<sub>5</sub> Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)
Fragment
screening of a thermostabilized mGlu<sub>5</sub> receptor
using a high-concentration radioligand binding assay enabled the identification
of moderate affinity, high ligand efficiency (LE) pyrimidine hit <b>5</b>. Subsequent optimization using structure-based drug discovery
methods led to the selection of <b>25</b>, HTL14242, as an advanced
lead compound for further development. Structures of the stabilized
mGlu<sub>5</sub> receptor complexed with <b>25</b> and another
molecule in the series, <b>14</b>, were determined at resolutions
of 2.6 and 3.1 Ă
, respectively