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  • Kyle Emmitte
2019

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

2 Scopus citations
1 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
2017

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

13 Scopus citations
2016

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 journalArticle

17 Scopus citations

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 journalArticle

5 Scopus citations

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 journalArticle

20 Scopus citations

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 article

80 Scopus citations

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 journalArticle

31 Scopus citations