Department of Pharmacology,
Vanderbilt Institute of Chemical Biology
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A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells.
Journal of biomolecular screening Dec, 2004 | Pubmed ID: 15634793
A novel high-throughput pepT1 transporter assay differentiates between substrates and antagonists.
Molecular pharmaceutics Jan, 2004 | Pubmed ID: 15832502
A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors.
Molecular pharmacology Apr, 2008 | Pubmed ID: 18171729
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.
Molecular pharmacology Nov, 2008 | Pubmed ID: 18664603
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
Bioorganic & medicinal chemistry letters Oct, 2008 | Pubmed ID: 18774291
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Bioorganic & medicinal chemistry letters Oct, 2008 | Pubmed ID: 18824351
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
Molecular pharmacology Mar, 2009 | Pubmed ID: 19047481
Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2.
Proceedings of the National Academy of Sciences of the United States of America Mar, 2009 | Pubmed ID: 19279215
Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
Journal of medicinal chemistry Jun, 2009 | Pubmed ID: 19438238
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.
Bioorganic & medicinal chemistry letters Jun, 2009 | Pubmed ID: 19443219
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
Journal of medicinal chemistry Jul, 2009 | Pubmed ID: 19469556
High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1.
Molecular pharmacology Nov, 2009 | Pubmed ID: 19706730
Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe.
Current topics in medicinal chemistry , 2009 | Pubmed ID: 19807667
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Bioorganic & medicinal chemistry letters Dec, 2009 | Pubmed ID: 19854049
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Bioorganic & medicinal chemistry letters Dec, 2009 | Pubmed ID: 19875287
Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7.
Molecular pharmacology Mar, 2010 | Pubmed ID: 20026717
Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening.
ACS chemical neuroscience Apr, 2010 | Pubmed ID: 20414370
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Bioorganic & medicinal chemistry letters Sep, 2010 | Pubmed ID: 20667732
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Molecular pharmacology Dec, 2010 | Pubmed ID: 20923853
Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel.
Molecular pharmacology Jan, 2011 | Pubmed ID: 20926757
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.
Bioorganic & medicinal chemistry letters May, 2011 | Pubmed ID: 21194936
Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells.
ACS chemical biology May, 2011 | Pubmed ID: 21241068
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.
Journal of medicinal chemistry Feb, 2011 | Pubmed ID: 21247167
Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay.
European journal of pharmacology Jun, 2011 | Pubmed ID: 21296065
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.
Bioorganic & medicinal chemistry letters Mar, 2011 | Pubmed ID: 21315585
Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGluâ‚„.
ACS combinatorial science Mar, 2011 | Pubmed ID: 21338051
High-throughput quantification of bioactive lipids by MALDI mass spectrometry: application to prostaglandins.
Analytical chemistry Sep, 2011 | Pubmed ID: 21770391
Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
The Journal of biological chemistry Sep, 2011 | Pubmed ID: 21795696
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.
ACS chemical neuroscience , 2010 | Pubmed ID: 21961051
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.
Journal of medicinal chemistry Nov, 2011 | Pubmed ID: 21966889
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Molecular pharmacology Feb, 2012 | Pubmed ID: 22021324
MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines.
Tetrahedron letters Jan, 2009 | Pubmed ID: 22090663
Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1.
Frontiers in pharmacology , 2011 | Pubmed ID: 22275899
The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.
ACS chemical neuroscience Dec, 2011 | Pubmed ID: 22368764
Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators.
Journal of molecular modeling Sep, 2012 | Pubmed ID: 22592386
A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer.
Nature chemical biology Jul, 2012 | Pubmed ID: 22634634
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.
Bioorganic & medicinal chemistry letters Jul, 2012 | Pubmed ID: 22727639
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Bioorganic & medicinal chemistry letters Oct, 2012 | Pubmed ID: 22981332
Identification and characterization of a compound that protects cardiac tissue from human Ether-Ã -go-go-related gene (hERG)-related drug-induced arrhythmias.
The Journal of biological chemistry Nov, 2012 | Pubmed ID: 23033485
Nonoisotopic assay for the presynaptic choline transporter reveals capacity for allosteric modulation of choline uptake.
ACS chemical neuroscience Oct, 2012 | Pubmed ID: 23077721
Benchmarking Ligand-Based Virtual High-Throughput Screening with the PubChem Database.
Molecules (Basel, Switzerland) , 2013 | Pubmed ID: 23299552
Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.
ACS medicinal chemistry letters Nov, 2010 | Pubmed ID: 23308336