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The publication data currently available has been vetted by Vanderbilt faculty, staff, administrators and trainees. The data itself is retrieved directly from NCBI's PubMed and is automatically updated on a weekly basis to ensure accuracy and completeness.

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Results: 1 to 10 of 239

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Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes.
Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2020) Bioorg Med Chem Lett 30: 126811
MeSH Terms: Allosteric Regulation, Animals, Drug Design, Half-Life, Humans, Inhibitory Concentration 50, Pyridazines, Quinazolines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship, Triazoles
Added March 3, 2020
0 Communities
1 Members
0 Resources
12 MeSH Terms
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M positive allosteric modulator (PAM) chemotype.
Temple KJ, Engers JL, Long MF, Watson KJ, Chang S, Luscombe VB, Jenkins MT, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2020) Bioorg Med Chem Lett 30: 126812
MeSH Terms: Allosteric Regulation, Drug Design, Drug Evaluation, Preclinical, Humans, Imidazoles, Kinetics, Protein Binding, Pyrazines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
10 MeSH Terms
Discovery of a novel 3,4-dimethylcinnoline carboxamide M positive allosteric modulator (PAM) chemotype via scaffold hopping.
Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 126678
MeSH Terms: Allosteric Regulation, Amides, Azetidines, Benzene, Molecular Structure, Protein Binding, Pyrazines, Pyridines, Pyrimidines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
11 MeSH Terms
Selective allosteric modulation of muscarinic acetylcholine receptors for the treatment of schizophrenia and substance use disorders.
Teal LB, Gould RW, Felts AS, Jones CK
(2019) Adv Pharmacol 86: 153-196
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Humans, Receptors, Muscarinic, Schizophrenia, Signal Transduction, Substance-Related Disorders
Added March 18, 2020
0 Communities
1 Members
0 Resources
8 MeSH Terms
VU6005806/AZN-00016130, an advanced M positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.
Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, Brandon NJ, Dugan ME, Niswender CM, Conn PJ, Bridges TM, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 1714-1718
MeSH Terms: Allosteric Regulation, Molecular Structure, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
4 MeSH Terms
Allosteric Regulation of Oligomerization by a B Trafficking G-Protein Is Corrupted in Methylmalonic Aciduria.
Ruetz M, Campanello GC, McDevitt L, Yokom AL, Yadav PK, Watkins D, Rosenblatt DS, Ohi MD, Southworth DR, Banerjee R
(2019) Cell Chem Biol 26: 960-969.e4
MeSH Terms: Allosteric Regulation, Amino Acid Metabolism, Inborn Errors, Fibroblasts, Guanosine Triphosphate, Humans, Methylmalonyl-CoA Mutase, Molecular Chaperones, Mutation, Protein Transport, Vitamin B 12
Added March 3, 2020
0 Communities
1 Members
0 Resources
10 MeSH Terms
Surveying heterocycles as amide bioisosteres within a series of mGlu NAMs: Discovery of VU6019278.
Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 1211-1214
MeSH Terms: Allosteric Regulation, Amides, Animals, Central Nervous System, Hepatocytes, Heterocyclic Compounds, Inhibitory Concentration 50, Pyrazoles, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).
Reed CW, Yohn SE, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW
(2019) J Med Chem 62: 1690-1695
MeSH Terms: Allosteric Regulation, Animals, Anti-Anxiety Agents, Benzamides, Brain, Drug Discovery, Male, Mice, Inbred C57BL, Molecular Structure, Rats, Sprague-Dawley, Receptors, Metabotropic Glutamate, Structure-Activity Relationship, Triazoles
Added March 3, 2020
0 Communities
1 Members
0 Resources
13 MeSH Terms
Novel M positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.
Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Conn PJ, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 362-366
MeSH Terms: Allosteric Regulation, Amides, Dose-Response Relationship, Drug, Humans, Hydrogen Bonding, Ligands, Molecular Structure, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate.
Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 342-346
MeSH Terms: Allosteric Regulation, Dose-Response Relationship, Drug, Drug Discovery, Heterocyclic Compounds, 2-Ring, Humans, Isoquinolines, Molecular Structure, Myotonin-Protein Kinase, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms