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  • Kyle Emmitte
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 journalArticle

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 journalArticle

3 Scopus citations

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 journalArticle

1 Scopus citations

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 journalArticle

5 Scopus citations

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 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 journalArticle

2 Scopus citations
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 journalArticle

1 Scopus citations

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 journalArticle

2 Scopus citations
2017

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 journalArticle

6 Scopus citations

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 journalArticle

13 Scopus citations

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 journalArticle

10 Scopus citations

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 journalArticle

1 Scopus citations

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 journalArticle

5 Scopus citations

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 journalArticle

13 Scopus citations

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 article

14 Scopus citations
2015

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 article

74 Scopus citations

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 journalArticle

18 Scopus citations

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 journalArticle

29 Scopus citations

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 journalArticle

55 Scopus citations

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., Feb 2015, In : Neuropsychopharmacology. 40, 3, p. 755-765 11 p.

Research output: Contribution to journalArticle

21 Scopus citations
2014

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 journalArticle

30 Scopus citations

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 journalArticle

7 Scopus citations

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 journalArticle

28 Scopus citations
2013

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 journalArticle

35 Scopus citations

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 journalArticle

23 Scopus citations

High-Throughput Screening for Modulators of the D2 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., 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 proceedingChapter

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 article

54 Scopus citations

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 journalArticle

9 Scopus citations

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 journalArticle

7 Scopus citations

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 journalArticle

11 Scopus citations
2012

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 article

163 Scopus citations

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 journalArticle

30 Scopus citations

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 journalArticle

14 Scopus citations

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 journalArticle

58 Scopus citations

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 journalArticle

29 Scopus citations
2011

(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 journalArticle

18 Scopus citations

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 article

54 Scopus citations
2010

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 journalArticle

18 Scopus citations