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2019

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Felts, A. S., Bollinger, K. A., Brassard, C. J., Rodriguez, A. L., Morrison, R. D., Scott Daniels, J., Blobaum, A. L., Niswender, C. M., Jones, C. K., Jeffrey Conn, P., Emmitte, K. A. & Lindsley, C. W., 1 Jan 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 1, p. 47-50 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Aldehyde Oxidase
Metabotropic Glutamate 5 Receptor
Metabotropic Glutamate Receptors
Metabolism
Modulators

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu 2 ) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores

Childress, E. S., Wieting, J. M., Felts, A. S., Breiner, M. M., Long, M. F., Luscombe, V. B., Rodriguez, A. L., Cho, H. P., Blobaum, A. L., Niswender, C. M., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 1 Oct 2019, In : Journal of Medicinal Chemistry. 62, 1, p. 378-384 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Rodentia
Central Nervous System
pyridine
pyrazolo(1,5-a)pyrimidine
metabotropic glutamate receptor 2

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M 1 Positive Allosteric Modulators

Engers, J. L., Bender, A. M., Kalbfleisch, J. J., Cho, H. P., Lingenfelter, K. S., Luscombe, V. B., Han, C., Melancon, B. J., Blobaum, A. L., Dickerson, J. W., Rook, J. M., Niswender, C. M., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1035-1042 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Lactams
Modulators
Cell Line
Muscarinic Receptors
Cells
3 Citations (Scopus)

Discovery of VU2957 (Valiglurax): An mGlu 4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease

Panarese, J. D., Engers, D. W., Wu, Y. J., Bronson, J. J., Macor, J. E., Chun, A., Rodriguez, A. L., Felts, A. S., Engers, J. L., Loch, M. T., Emmitte, K. A., Castelhano, A. L., Kates, M. J., Nader, M. A., Jones, C. K., Blobaum, A. L., Conn, P. J., Niswender, C. M., Hopkins, C. R. & Lindsley, C. W., 14 Mar 2019, In : ACS Medicinal Chemistry Letters. 10, 3, p. 255-260 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Pulse amplitude modulation
Toxicology
Modulators
Parkinson Disease
Pharmacology
1 Citation (Scopus)

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu 4 PAM development candidate

Panarese, J. D., Engers, D. W., Wu, Y. J., Guernon, J. M., Chun, A., Gregro, A. R., Bender, A. M., Capstick, R. A., Wieting, J. M., Bronson, J. J., Macor, J. E., Westphal, R., Soars, M., Engers, J. E., Felts, A. S., Rodriguez, A. L., Emmitte, K. A., Jones, C. K., Blobaum, A. L., Jeffrey Conn, P. & 3 others, Niswender, C. M., Hopkins, C. R. & Lindsley, C. W., 15 Jan 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 2, p. 342-346 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulators
2018

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Blobaum, A. L., Byers, F. W., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Jun 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 10, p. 1679-1685 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Metabotropic Glutamate Receptors
Modulators
Assays
Metabolism

Stress and interferon signalling-mediated apoptosis contributes to pleiotropic anticancer responses induced by targeting NGLY1

Zolekar, A., Lin, V. J. T., Mishra, N. M., Ho, Y. Y., Hayatshahi, H. S., Parab, A., Sampat, R., Liao, X., Hoffmann, P., Liu, J., Emmitte, K. A. & Wang, Y-C., 11 Dec 2018, In : British Journal of Cancer. 119, 12, p. 1538-1551 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Interferons
Melanoma
Apoptosis
Neoplasms
Systems Biology
2017
4 Citations (Scopus)

Co-activation of metabotropic glutamate receptor 3 and beta-adrenergic receptors modulates cyclic-AMP and long-term potentiation, and disrupts memory reconsolidation

Walker, A. G., Sheffler, D. J., Lewis, A. S., Dickerson, J. W., Foster, D. J., Senter, R. K., Moehle, M. S., Lv, X., Stansley, B. J., Xiang, Z., Rook, J. M., Emmitte, K. A., Lindsley, C. W. & Conn, P. J., 1 Dec 2017, In : Neuropsychopharmacology. 42, 13, p. 2553-2566 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Long-Term Potentiation
Receptors, Adrenergic, beta
Cyclic AMP
Glutamic Acid
Adrenergic Receptors
7 Citations (Scopus)

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core

Bollinger, K. A., Felts, A. S., Brassard, C. J., Engers, J. L., Rodriguez, A. L., Weiner, R. L., Cho, H. P., Chang, S., Bubser, M., Jones, C. K., Blobaum, A. L., Niswender, C. M., Conn, P. J., Emmitte, K. A. & Lindsley, C. W., 1 Jan 2017, In : ACS Medicinal Chemistry Letters. 8, 9, p. 919-924 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Neurology
Modulators
Inhibitory Concentration 50
Central Nervous System
Scaffolds
7 Citations (Scopus)

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

Engers, J. L., Bollinger, K. A., Weiner, R. L., Rodriguez, A. L., Long, M. F., Breiner, M. M., Chang, S., Bollinger, S. R., Bubser, M., Jones, C. K., Morrison, R. D., Bridges, T. M., Blobaum, A. L., Niswender, C. M., Conn, P. J., Emmitte, K. A. & Lindsley, C. W., 1 Jan 2017, In : ACS Medicinal Chemistry Letters. 8, 9, p. 925-930 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Pyridones
Neurology
Scaffolds
Inhibitory Concentration 50
Rats
1 Citation (Scopus)

Development and kilogram-scale synthesis of mGlu5 negative allosteric modulator VU0424238 (auglurant)

David, T. K., Prashanth, N. K., Rajendraswami, M., Pallalu, D., Castelhano, A. L., Kates, M. J., Blobaum, A. L., Jones, C. K., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 6 Sep 2017, In : Tetrahedron Letters. 58, 36, p. 3554-3558 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Pharmaceutical Chemistry
Chromatography
Silicon Dioxide
Toxicology
Modulators
5 Citations (Scopus)

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Bollinger, K. A., Venable, D. F., Blobaum, A. L., Byers, F. W., Thompson Gray, A., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Nov 2017, In : Bioorganic and Medicinal Chemistry Letters. 27, 21, p. 4858-4866 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Dopamine Plasma Membrane Transport Proteins
Metabotropic Glutamate Receptors
Modulators
Pharmacokinetics
10 Citations (Scopus)

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

Felts, A. S., Rodriguez, A. L., Blobaum, A. L., Morrison, R. D., Bates, B. S., Thompson Gray, A., Rook, J. M., Tantawy, M. N., Byers, F. W., Chang, S., Venable, D. F., Luscombe, V. B., Tamagnan, G. D., Niswender, C. M., Daniels, J. S., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 22 Jun 2017, In : Journal of Medicinal Chemistry. 60, 12, p. 5072-5085 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Allosteric Site
Macaca fascicularis
Papio
Neurodegenerative Diseases
11 Citations (Scopus)

mGlu5 negative allosteric modulators: a patent review (2013 - 2016)

Emmitte, K. A., 3 Jun 2017, In : Expert Opinion on Therapeutic Patents. 27, 6, p. 691-706 16 p.

Research output: Contribution to journalReview articleResearchpeer-review

Alkynes
Clinical Trials
Expert Testimony
Research
Neurodegenerative Diseases
2016
15 Citations (Scopus)

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

Wood, M. R., Noetzel, M. J., Engers, J. L., Bollinger, K. A., Melancon, B. J., Tarr, J. C., Han, C., West, M., Gregro, A. R., Lamsal, A., Chang, S., Ajmera, S., Smith, E., Chase, P., Hodder, P. S., Bubser, M., Jones, C. K., Hopkins, C. R., Emmitte, K. A., Niswender, C. M. & 5 others, Wood, M. W., Duggan, M. E., Conn, P. J., Bridges, T. M. & Lindsley, C. W., 1 Jul 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 13, p. 3029-3033 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulators
Rats
Brain
Muscarinic Receptors
Plasmas
6 Citations (Scopus)

Evaluating the disposition of a mixed aldehyde oxidase/cytochrome P450 substrate in rats with attenuated P450 activity

Crouch, R. D., Morrison, R. D., Byers, F. W., Lindsley, C. W., Emmitte, K. A. & Daniels, J. S., 1 Aug 2016, In : Drug Metabolism and Disposition. 44, 8, p. 1296-1303 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Aldehyde Oxidase
Cytochrome P-450 Enzyme System
Drug Interactions
NADP
Area Under Curve
3 Citations (Scopus)

N-Alkylpyrido[1′,2′:1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Venable, D. F., Blobaum, A. L., Byers, F. W., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 15 Apr 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 8, p. 1894-1900 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate Receptors
Pharmaceutical Chemistry
Central Nervous System Diseases
Neurology
Modulators
19 Citations (Scopus)

Partial mGlu 5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

Gould, R. W., Amato, R. J., Bubser, M., Joffe, M. E., Nedelcovych, M. T., Thompson, A. D., Nickols, H. H., Yuh, J. P., Zhan, X., Felts, A. S., Rodriguez, A. L., Morrison, R. D., Byers, F. W., Rook, J. M., Daniels, J. S., Niswender, C. M., Conn, P. J., Emmitte, K. A., Lindsley, C. W. & Jones, C. K., 1 Mar 2016, In : Neuropsychopharmacology. 41, 4, p. 1166-1178 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Cocaine
Cocaine-Related Disorders
Therapeutics
Self Administration
63 Citations (Scopus)

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

Lindsley, C. W., Emmitte, K. A., Hopkins, C. R., Bridges, T. M., Gregory, K. J., Niswender, C. M. & Conn, P. J., 8 Jun 2016, In : Chemical Reviews. 116, 11, p. 6707-6741 35 p.

Research output: Contribution to journalReview articleResearchpeer-review

Metabotropic Glutamate Receptors
Modulators
Ligands
Metabolism
Conformations
22 Citations (Scopus)

Targeting BRCA1-and BRCA2-deficient cells with RAD52 small molecule inhibitors

Huang, F., Goyal, N., Sullivan, K., Hanamshet, K., Patel, M., Mazina, O. M., Wang, C. X., An, W. F., Spoonamore, J., Metkar, S., Emmitte, K. A., Cocklin, S., Skorski, T. & Mazin, A. V., 19 May 2016, In : Nucleic Acids Research. 44, 9, p. 4189-4199 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Mutation
Homologous Recombination
DNA Repair
Ovarian Neoplasms
Libraries
20 Citations (Scopus)

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

Nickols, H. H., Yuh, J. P., Gregory, K. J., Morrison, R. D., Bates, B. S., Stauffer, S. R., Emmitte, K. A., Bubser, M., Peng, W., Nedelcovych, M. T., Thompson, A., Lv, X., Xiang, Z., Daniels, J. S., Niswender, C. M., Lindsley, C. W., Jones, C. K. & Conn, P. J., 1 Jan 2016, In : The Journal of pharmacology and experimental therapeutics. 356, 1, p. 123-136 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Central Nervous System
Allosteric Site
Fragile X Syndrome
Inositol Phosphates
2015
70 Citations (Scopus)

Advancing biological understanding and therapeutics discovery with small-molecule probes

Schreiber, S. L., Kotz, J. D., Li, M., Aubé, J., Austin, C. P., Reed, J. C., Rosen, H., White, E. L., Sklar, L. A., Lindsley, C. W., Alexander, B. R., Bittker, J. A., Clemons, P. A., De Souza, A., Foley, M. A., Palmer, M., Shamji, A. F., Wawer, M. J., McManus, O., Wu, M. & 26 others, Zou, B., Yu, H., Golden, J. E., Schoenen, F. J., Simeonov, A., Jadhav, A., Jackson, M. R., Pinkerton, A. B., Chung, T. D. Y., Griffin, P. R., Cravatt, B. F., Hodder, P. S., Roush, W. R., Roberts, E., Chung, D. H., Jonsson, C. B., Noah, J. W., Severson, W. E., Ananthan, S., Edwards, B., Oprea, T. I., Conn, P. J., Hopkins, C. R., Wood, M. R., Stauffer, S. R. & Emmitte, K. A., 1 Jan 2015, In : Cell. 161, 6, p. 1252-1265 14 p.

Research output: Contribution to journalReview articleResearchpeer-review

Molecules
Biological Phenomena
Therapeutics
Biological systems
Medicine
15 Citations (Scopus)

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Felts, A. S., Rodriguez, A. L., Smith, K. A., Engers, J. L., Morrison, R. D., Byers, F. W., Blobaum, A. L., Locuson, C. W., Chang, S., Venable, D. F., Niswender, C. M., Daniels, J. S., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 25 Nov 2015, In : Journal of Medicinal Chemistry. 58, 22, p. 9027-9040 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate Receptors
Literature
Patents
Central Nervous System Diseases
Muscarinic Receptors
25 Citations (Scopus)

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

Engers, J. L., Rodriguez, A. L., Konkol, L. C., Morrison, R. D., Thompson, A. D., Byers, F. W., Blobaum, A. L., Chang, S., Venable, D. F., Loch, M. T., Niswender, C. M., Daniels, J. S., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 24 Sep 2015, In : Journal of Medicinal Chemistry. 58, 18, p. 7485-7500 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate Receptors
Anti-Anxiety Agents
Antidepressive Agents
Rodentia
Pyrazines
48 Citations (Scopus)

Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction

Walker, A. G., Wenthur, C. J., Xiang, Z., Rook, J. M., Emmitte, K. A., Niswender, C. M., Lindsley, C. W. & Conn, P. J., 27 Jan 2015, In : Proceedings of the National Academy of Sciences of the United States of America. 112, 4, p. 1196-1201 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Prefrontal Cortex
Fear
Depression
Cognition
Bipolar Disorder
18 Citations (Scopus)

Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles

Rook, J. M., Tantawy, M. N., Ansari, M. S., Felts, A. S., Stauffer, S. R., Emmitte, K. A., Kessler, R. M., Niswender, C. M., Daniels, J. S., Jones, C. K., Lindsley, C. W. & Conn, P. J., 1 Jan 2015, In : Neuropsychopharmacology. 40, 3, p. 755-765 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Positron-Emission Tomography
Allosteric Site
Ligands
Brain Diseases
2014
28 Citations (Scopus)

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors

Cho, H. P., Engers, D. W., Venable, D. F., Niswender, C. M., Lindsley, C. W., Conn, P. J., Emmitte, K. A. & Rodriguez, A. L., 16 Jul 2014, In : ACS Chemical Neuroscience. 5, 7, p. 597-610 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate Receptors
Modulators
Rats
Human Activities
High-Throughput Screening Assays
7 Citations (Scopus)

Discovery of VU0431316: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

Bates, B. S., Rodriguez, A. L., Felts, A. S., Morrison, R. D., Venable, D. F., Blobaum, A. L., Byers, F. W., Lawson, K. P., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Aug 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 15, p. 3307-3314 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulators
Anxiety
Allosteric Site
Pyrazines
Calcium Carbonate
26 Citations (Scopus)

Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site

Gregory, K. J., Nguyen, E. D., Malosh, C., Mendenhall, J. L., Zic, J. Z., Bates, B. S., Noetzel, M. J., Squire, E. F., Turner, E. M., Rook, J. M., Emmitte, K. A., Stauffer, S. R., Lindsley, C. W., Meiler, J. & Conn, P. J., 16 Apr 2014, In : ACS Chemical Neuroscience. 5, 4, p. 282-295 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Allosteric Site
Scaffolds
Modulators
Ligands
2013
31 Citations (Scopus)

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)

Wenthur, C. J., Morrison, R., Felts, A. S., Smith, K. A., Engers, J. L., Byers, F. W., Daniels, J. S., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 27 Jun 2013, In : Journal of Medicinal Chemistry. 56, 12, p. 5208-5212 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Inhibitory Concentration 50
Deuterium
(R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl)(3-hydroxypiperidin-1-yl)methanone
In Vitro Techniques
22 Citations (Scopus)

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Venable, D. F., Manka, J. T., Bates, B. S., Blobaum, A. L., Byers, F. W., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Nov 2013, In : Bioorganic and Medicinal Chemistry Letters. 23, 21, p. 5779-5785 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulators
Anxiety
Allosteric Site
Calcium Carbonate
Anti-Anxiety Agents

High-Throughput Screening for Modulators of the D 2 Dopamine Receptor Yields Unique and Selective Pharmacological Chemotypes

Free, R. B., Conroy, J. L., Roof, R. A., Doyle, T., Han, Y., Donthamsetti, P., Javitch, J. A., Southall, N., Emmitte, K. A., Lindsley, C., Ferrer, M. & Sibley, D. R., 1 Dec 2013, Catecholamine Research in the 21st Century: Abstracts and Graphical Abstracts, 10th International Catecholamine Symposium, 2012. Elsevier Inc., 1 p.

Research output: Chapter in Book/Report/Conference proceedingChapterResearchpeer-review

Dopamine Receptors
Pharmacology
53 Citations (Scopus)

MGlu5 negative allosteric modulators: A patent review (2010-2012)

Emmitte, K. A., 1 Apr 2013, In : Expert Opinion on Therapeutic Patents. 23, 4, p. 393-408 16 p.

Research output: Contribution to journalReview articleResearchpeer-review

Alkynes
Metabotropic Glutamate 5 Receptor
Pharmaceutical Preparations
Fragile X Syndrome
Dyskinesias
9 Citations (Scopus)

N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats

Lovell, K. M., Felts, A. S., Rodriguez, A. L., Venable, D. F., Cho, H. P., Morrison, R. D., Byers, F. W., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Jul 2013, In : Bioorganic and Medicinal Chemistry Letters. 23, 13, p. 3713-3718 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulators
Rats
Assays
Protein Binding
Pharmacokinetics
7 Citations (Scopus)

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu 1

Manka, J. T., Rodriguez, A. L., Morrison, R. D., Venable, D. F., Cho, H. P., Blobaum, A. L., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 15 Sep 2013, In : Bioorganic and Medicinal Chemistry Letters. 23, 18, p. 5091-5096 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulators
Assays
Protein Binding
Scaffolds
Pharmaceutical Preparations
9 Citations (Scopus)

Substituted 1-phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: Discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction

Amato, R. J., Felts, A. S., Rodriguez, A. L., Venable, D. F., Morrison, R. D., Byers, F. W., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W., Jones, C. K. & Emmitte, K. A., 21 Aug 2013, In : ACS Chemical Neuroscience. 4, 8, p. 1217-1228 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Cocaine-Related Disorders
Cocaine
Modulators
Urea
Rats
2012
161 Citations (Scopus)

Allosteric modulation of seven transmembrane spanning receptors: Theory, practice, and opportunities for central nervous system drug discovery

Melancon, B. J., Hopkins, C. R., Wood, M. R., Emmitte, K. A., Niswender, C. M., Christopoulos, A., Conn, P. J. & Lindsley, C. W., 23 Feb 2012, In : Journal of Medicinal Chemistry. 55, 4, p. 1445-1464 20 p.

Research output: Contribution to journalReview articleResearchpeer-review

Allosteric Regulation
Central Nervous System Agents
Metabotropic Glutamate Receptors
Muscarinic Receptors
Drug Discovery
27 Citations (Scopus)

Discovery of 2-(2-Benzoxazoyl amino)-4-Aryl-5-Cyanopyrimidine as Negative Allosteric Modulators (NAMs) of Metabotropic Glutamate Receptor5 (mGlu 5): From an Artificial Neural Network Virtual Screen to an In Vivo Tool Compound

Mueller, R., Dawson, E. S., Meiler, J., Rodriguez, A. L., Chauder, B. A., Bates, B. S., Felts, A. S., Lamb, J. P., Menon, U. N., Jadhav, S. B., Kane, A. S., Jones, C. K., Gregory, K. J., Niswender, C. M., Conn, P. J., Olsen, C. M., Winder, D. G., Emmitte, K. A. & Lindsley, C. W., 5 Mar 2012, In : ChemMedChem. 7, 3, p. 406-414 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Benzoxazoles
Allosteric Regulation
High-Throughput Screening Assays
Small Molecule Libraries
Pyrimidines
13 Citations (Scopus)

Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway

Theriault, J. R., Felts, A. S., Bates, B. S., Perez, J. R., Palmer, M., Gilbert, S. R., Dawson, E. S., Engers, J. L., Lindsley, C. W. & Emmitte, K. A., 1 Jan 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 1, p. 76-81 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular Probes
Genes
Chemical activation
Musculoskeletal system
Triazines
55 Citations (Scopus)

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: Enriching structure-function studies and structure-activity relationships

Gregory, K. J., Noetzel, M. J., Rook, J. M., Vinson, P. N., Stauffer, S. R., Rodriguez, A. L., Emmitte, K. A., Zhou, Y., Chun, A. C., Felts, A. S., Chauder, B. A., Lindsley, C. W., Niswender, C. M. & Conn, P. J., 1 Nov 2012, In : Molecular Pharmacology. 82, 5, p. 860-875 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Structure-Activity Relationship
Allosteric Site
G-Protein-Coupled Receptors
Ligands
25 Citations (Scopus)

The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5

Morrison, R. D., Blobaum, A. L., Byers, F. W., Santomango, T. S., Bridges, T. M., Stec, D., Brewer, K. A., Sanchez-Ponce, R., Corlew, M. M., Rush, R., Felts, A. S., Manka, J., Bates, B. S., Venable, D. F., Rodriguez, A. L., Jones, C. K., Niswender, C. M., Conn, P. J., Lindsley, C. W., Emmitte, K. A. & 1 others, Daniels, J. S., 1 Sep 2012, In : Drug Metabolism and Disposition. 40, 9, p. 1834-1845 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Aldehyde Oxidase
Metabotropic Glutamate 5 Receptor
Xanthine Oxidase
Biotransformation
Mixed Function Oxygenases
2011
18 Citations (Scopus)

(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu5: Discovery of a new tool compound with activity in the OSS mouse model of addiction

Lindsley, C. W., Bates, B. S., Menon, U. N., Jadhav, S. B., Kane, A. S., Jones, C. K., Rodriguez, A. L., Conn, P. J., Olsen, C. M., Winder, D. G. & Emmitte, K. A., 17 Aug 2011, In : ACS Chemical Neuroscience. 2, 8, p. 471-482 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabotropic Glutamate Receptors
Modulators
Assays
Anxiety
Ionotropic Glutamate Receptors
54 Citations (Scopus)

Recent advances in the design and development of novel negative allosteric modulators of mGlu 5

Emmitte, K. A., 17 Aug 2011, In : ACS Chemical Neuroscience. 2, 8, p. 411-432 22 p.

Research output: Contribution to journalReview articleResearchpeer-review

Metabotropic Glutamate 5 Receptor
Metabotropic Glutamate Receptors
Modulators
Literature
Fragile X Syndrome
2010
17 Citations (Scopus)

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu 5: Identification of easily prepared tool compounds with CNS exposure in rats

Felts, A. S., Lindsley, S. R., Lamb, J. P., Rodriguez, A. L., Menon, U. N., Jadhav, S., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Aug 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 15, p. 4390-4394 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Protein Binding
Modulators
Rats
Assays
Pharmacokinetics