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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: 11 to 20 of 613

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Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy.
Yamada Y, Yohn SE, Gilliland K, Loch MT, Schulte ML, Rodriguez AL, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 2670-2674
MeSH Terms: Animals, Anti-Anxiety Agents, Antidepressive Agents, Dose-Response Relationship, Drug, Mice, Molecular Structure, Pyridones, Rats, Receptors, Metabotropic Glutamate, Stereoisomerism, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
11 MeSH Terms
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M PAMs.
Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, Daniels JS, Stec DF, Niswender CM, Jones CK, Wood MR, Wood MW, Duggan ME, Brandon NJ, Conn PJ, Bridges TM, Lindsley CW, Melancon BJ
(2019) Bioorg Med Chem Lett 29: 2224-2228
MeSH Terms: Aldehyde Oxidase, Animals, Drug Discovery, Humans, Myotonia Congenita, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
3 Members
0 Resources
8 MeSH Terms
Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063.
Kharade SV, Sanchez-Andres JV, Fulton MG, Shelton EL, Blobaum AL, Engers DW, Hofmann CS, Dadi PK, Lantier L, Jacobson DA, Lindsley CW, Denton JS
(2019) J Pharmacol Exp Ther 370: 350-359
MeSH Terms: Animals, Ductus Arteriosus, Glucose, HEK293 Cells, Humans, Insulin Secretion, Insulin-Secreting Cells, Ion Channel Gating, Mice, Potassium Channels, Inwardly Rectifying, Structure-Activity Relationship, Sulfonylurea Receptors, Vasodilation, Xanthines
Added June 14, 2021
0 Communities
1 Members
0 Resources
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
BCL::Mol2D-a robust atom environment descriptor for QSAR modeling and lead optimization.
Vu O, Mendenhall J, Altarawy D, Meiler J
(2019) J Comput Aided Mol Des 33: 477-486
MeSH Terms: Algorithms, Drug Design, Drug Discovery, Humans, Ligands, Quantitative Structure-Activity Relationship, Small Molecule Libraries
Added March 21, 2020
0 Communities
1 Members
0 Resources
7 MeSH Terms
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW
(2019) J Med Chem 62: 3971-3988
MeSH Terms: Animals, Antineoplastic Agents, Azepines, Binding Sites, Cell Line, Tumor, Cell Survival, Crystallography, X-Ray, Drug Evaluation, Preclinical, Female, Humans, Mice, Mice, Inbred NOD, Mice, SCID, Molecular Dynamics Simulation, Myeloid Cell Leukemia Sequence 1 Protein, Neoplasms, Protein Structure, Tertiary, Small Molecule Libraries, Structure-Activity Relationship, Xenograft Model Antitumor Assays
Added April 15, 2019
0 Communities
1 Members
0 Resources
20 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
Maturation of the respiratory complex II flavoprotein.
Sharma P, Maklashina E, Cecchini G, Iverson TM
(2019) Curr Opin Struct Biol 59: 38-46
MeSH Terms: Animals, Cell Respiration, Electron Transport Chain Complex Proteins, Electron Transport Complex II, Flavin-Adenine Dinucleotide, Flavoproteins, Humans, Protein Binding, Protein Subunits, Structure-Activity Relationship
Added April 1, 2019
0 Communities
1 Members
0 Resources
10 MeSH Terms
On-target Resistance to the Mutant-Selective EGFR Inhibitor Osimertinib Can Develop in an Allele-Specific Manner Dependent on the Original EGFR-Activating Mutation.
Brown BP, Zhang YK, Westover D, Yan Y, Qiao H, Huang V, Du Z, Smith JA, Ross JS, Miller VA, Ali S, Bazhenova L, Schrock AB, Meiler J, Lovly CM
(2019) Clin Cancer Res 25: 3341-3351
MeSH Terms: Acrylamides, Alleles, Aniline Compounds, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Dose-Response Relationship, Drug, Drug Resistance, Neoplasm, ErbB Receptors, Exons, Gene Expression Profiling, Humans, Lung Neoplasms, Models, Molecular, Mutation, Protein Binding, Protein Kinase Inhibitors, Structure-Activity Relationship
Added March 21, 2020
0 Communities
2 Members
0 Resources
17 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