Search Results - "Watson, Katherine J."

Discovery of structurally distinct tricyclic M 4 positive allosteric modulator (PAM) chemotypes by Temple, Kayla J, Long, Madeline F, Engers, Julie L, Watson, Katherine J, Chang, Sichen, Luscombe, Vincent B, Rodriguez, Alice L, Niswender, Colleen M, Bridges, Thomas M, Conn, P Jeffrey, Engers, Darren W, Lindsley, Craig W

“…This Letter details our efforts to develop new M PAM scaffolds with improved pharmacological properties. This endeavor involved replacing the…”
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Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping by Temple, Kayla J., Engers, Julie L., Long, Madeline F., Gregro, Alison R., Watson, Katherine J., Chang, Sichen, Jenkins, Matthew T., Luscombe, Vincent B., Rodriguez, Alice L., Niswender, Colleen M., Bridges, Thomas M., Conn, P. Jeffrey, Engers, Darren W., Lindsley, Craig W.

“…[Display omitted] •Novel 2.4-dimehtylcinnoline-based M4 PAMs.•Utility of scaffold hopping to improve properties/DMPK.•Balanced human and rat M4 PAM potency…”
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Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M 4 positive allosteric modulator (PAM) chemotype by Temple, Kayla J, Engers, Julie L, Long, Madeline F, Watson, Katherine J, Chang, Sichen, Luscombe, Vincent B, Jenkins, Matthew T, Rodriguez, Alice L, Niswender, Colleen M, Bridges, Thomas M, Conn, P Jeffrey, Engers, Darren W, Lindsley, Craig W

“…This Letter details our efforts to discover structurally unique M PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of…”
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Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes by Temple, Kayla J., Long, Madeline F., Engers, Julie L., Watson, Katherine J., Chang, Sichen, Luscombe, Vincent B., Rodriguez, Alice L., Niswender, Colleen M., Bridges, Thomas M., Conn, P. Jeffrey, Engers, Darren W., Lindsley, Craig W.

“…[Display omitted] •Discovery of novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide-based M4 PAMs.•Broad survey of diverse heterocyclic cores.•Balanced…”
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Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype by Temple, Kayla J., Engers, Julie L., Long, Madeline F., Watson, Katherine J., Chang, Sichen, Luscombe, Vincent B., Jenkins, Matthew T., Rodriguez, Alice L., Niswender, Colleen M., Bridges, Thomas M., Conn, P. Jeffrey, Engers, Darren W., Lindsley, Craig W.

“…[Display omitted] •Discovery of two novel tricyclic-based M4 PAMs.•Utility of scaffold hopping to improve potency/properties/DMPK.•Balanced human and rat M4…”
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Discovery of VU6028418: A Highly Selective and Orally Bioavailable M 4 Muscarinic Acetylcholine Receptor Antagonist by Spock, Matthew, Carter, Trever R, Bollinger, Katrina A, Han, Changho, Baker, Logan A, Rodriguez, Alice L, Peng, Li, Dickerson, Jonathan W, Qi, Aidong, Rook, Jerri M, O'Neill, Jordan C, Watson, Katherine J, Chang, Sichen, Bridges, Thomas M, Engers, Julie L, Engers, Darren W, Niswender, Colleen M, Conn, P Jeffrey, Lindsley, Craig W, Bender, Aaron M

“…Herein, we report the SAR leading to the discovery of VU6028418, a potent M mAChR antagonist with high subtype-selectivity and attractive DMPK properties and…”
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Development of a Peripherally Restricted 5-HT2B Partial Agonist for Treatment of Pulmonary Arterial Hypertension by Valentine, Michael S., Bender, Aaron M., Shay, Sheila, Paffenroth, Krista C., Gladson, Santhi, Dickerson, Jonathan W., Watson, Katherine J., Kapolka, Nicholas J., Boutaud, Olivier, Rook, Jerri M., Blackwell, Timothy S., Roth, Bryan L., Harrison, Fiona E., Austin, Eric D., West, James D., Lindsley, Craig W., Merryman, W. David

“…Ligands for the serotonin 2B receptor (5-HT2B) have shown potential to treat pulmonary arterial hypertension in preclinical models but cannot be used in humans…”
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Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist by Spock, Matthew, Carter, Trever R, Bollinger, Katrina A, Han, Changho, Baker, Logan A, Rodriguez, Alice L, Peng, Li, Dickerson, Jonathan W, Qi, Aidong, Rook, Jerri M, O’Neill, Jordan C, Watson, Katherine J, Chang, Sichen, Bridges, Thomas M, Engers, Julie L, Engers, Darren W, Niswender, Colleen M, Conn, P. Jeffrey, Lindsley, Craig W, Bender, Aaron M

“…Herein, we report the SAR leading to the discovery of VU6028418, a potent M4 mAChR antagonist with high subtype-selectivity and attractive DMPK properties in…”
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Discovery of the First Selective M 4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy by Moehle, Mark S, Bender, Aaron M, Dickerson, Jonathan W, Foster, Daniel J, Qi, Aidong, Cho, Hyekyung P, Donsante, Yuping, Peng, Weimin, Bryant, Zoey, Stillwell, Kaylee J, Bridges, Thomas M, Chang, Sichen, Watson, Katherine J, O'Neill, Jordan C, Engers, Julie L, Peng, Li, Rodriguez, Alice L, Niswender, Colleen M, Lindsley, Craig W, Hess, Ellen J, Conn, P Jeffrey, Rook, Jerri M

“…Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some…”
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Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy by Moehle, Mark S, Bender, Aaron M, Dickerson, Jonathan W, Foster, Daniel J, Qi, Aidong, Cho, Hyekyung P, Donsante, Yuping, Peng, Weimin, Bryant, Zoey, Stillwell, Kaylee J, Bridges, Thomas M, Chang, Sichen, Watson, Katherine J, O’Neill, Jordan C, Engers, Julie L, Peng, Li, Rodriguez, Alice L, Niswender, Colleen M, Lindsley, Craig W, Hess, Ellen J, Conn, P. Jeffrey, Rook, Jerri M

“…Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some…”
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Development of a Peripherally Restricted 5-HT 2B Partial Agonist for Treatment of Pulmonary Arterial Hypertension by Valentine, Michael S, Bender, Aaron M, Shay, Sheila, Paffenroth, Krista C, Gladson, Santhi, Dickerson, Jonathan W, Watson, Katherine J, Kapolka, Nicholas J, Boutaud, Olivier, Rook, Jerri M, Blackwell, Timothy S, Roth, Bryan L, Harrison, Fiona E, Austin, Eric D, West, James D, Lindsley, Craig W, Merryman, W David

“…Ligands for the serotonin 2B receptor (5-HT ) have shown potential to treat pulmonary arterial hypertension in preclinical models but cannot be used in humans…”
Get full text