• 3017 Citations
  • 31 h-Index
19992020

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Research Output

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Article
2012

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

Salovich, J. M., Vinson, P. N., Sheffler, D. J., Lamsal, A., Utley, T. J., Blobaum, A. L., Bridges, T. M., Le, U., Jones, C. K., Wood, M. R., Scott Daniels, J., Jeffrey Conn, P., Niswender, C. M., Lindsley, C. W. & Hopkins, C. R., Aug 1 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 15, p. 5084-5088 5 p.

Research output: Contribution to journalArticle

29 Scopus citations

DMH1, a highly selective small molecule BMP inhibitor promotes neurogenesis of hiPSCs: Comparison of PAX6 and SOX1 expression during neural induction

Neely, M. D., Litt, M. J., Tidball, A. M., Li, G. G., Aboud, A. A., Hopkins, C. R., Chamberlin, R., Hong, C. C., Ess, K. C. & Bowman, A. B., Jun 20 2012, In : ACS Chemical Neuroscience. 3, 6, p. 482-491 10 p.

Research output: Contribution to journalArticle

57 Scopus citations

DMH1, a novel BMP small molecule inhibitor, increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells

Ao, A., Hao, J., Hopkins, C. R. & Hong, C. C., Jul 27 2012, In : PloS one. 7, 7, e41627.

Research output: Contribution to journalArticle

35 Scopus citations

Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias

Potet, F., Lorinc, A. N., Chaigne, S., Hopkins, C. R., Venkataraman, R., Stepanovic, S. Z., Lewis, L. M., Days, E., Sidorov, V. Y., Engers, D. W., Zou, B., Afshartous, D., George, A. L., Campbell, C. M., Balser, J. R., Li, M., Baudenbacher, F. J., Lindsley, C. W., Weaver, C. D. & Kupershmidt, S., Nov 16 2012, In : Journal of Biological Chemistry. 287, 47, p. 39613-39625 13 p.

Research output: Contribution to journalArticle

11 Scopus citations

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1- tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K v7.1 (KCNQ1) potassium channel activator

Mattmann, M. E., Yu, H., Lin, Z., Xu, K., Huang, X., Long, S., Wu, M., McManus, O. B., Engers, D. W., Le, U. M., Li, M., Lindsley, C. W. & Hopkins, C. R., Sep 15 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 18, p. 5936-5941 6 p.

Research output: Contribution to journalArticle

28 Scopus citations

Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators

Mueller, R., Dawson, E. S., Niswender, C. M., Butkiewicz, M., Hopkins, C. R., Weaver, C. D., Lindsley, C. W., Conn, P. J. & Meiler, J., Sep 2012, In : Journal of Molecular Modeling. 18, 9, p. 4437-4446 10 p.

Research output: Contribution to journalArticle

9 Scopus citations

The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease

Jones, C. K., Bubser, M., Thompson, A. D., Dickerson, J. W., Turle-Lorenzo, N., Amalric, M., Blobaum, A. L., Bridges, T. M., Morrison, R. D., Jadhav, S., Engers, D. W., Italiano, K., Bode, J., Daniels, J. S., Lindsley, C. W., Hopkins, C. R., Conn, P. J. & Niswender, C. M., Feb 2012, In : Journal of Pharmacology and Experimental Therapeutics. 340, 2, p. 404-421 18 p.

Research output: Contribution to journalArticle

71 Scopus citations
2011

ACS chemical neuroscience molecule spotlight on gilenya (fingolimod; FTY720)

Hopkins, C. R., Mar 16 2011, In : ACS Chemical Neuroscience. 2, 3, p. 116-117 2 p.

Research output: Contribution to journalArticle

3 Scopus citations

ACS chemical neuroscience molecule spotlight on RG1678

Hopkins, C. R., Dec 21 2011, In : ACS Chemical Neuroscience. 2, 12, p. 685-686 2 p.

Research output: Contribution to journalArticle

11 Scopus citations

ACS chemical neuroscience molecule spotlight on Viibryd (vilazodone)

Hopkins, C. R., Oct 19 2011, In : ACS Chemical Neuroscience. 2, 10, 1 p.

Research output: Contribution to journalArticle

9 Scopus citations

Application of small organic molecules reveals cooperative TGFβ and BMP regulation of mesothelial cell behaviors

Cross, E. E., Thomason, R. T., Martinez, M., Hopkins, C. R., Hong, C. C. & Bader, D. M., Sep 2 2011, In : ACS chemical biology. 6, 9, p. 952-961 10 p.

Research output: Contribution to journalArticle

15 Scopus citations

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

Raphemot, R., Lonergan, D. F., Nguyen, T. T., Utley, T., Michelle Lewis, L., Kadakia, R., David Weaver, C., Gogliotti, R., Hopkins, C., Lindsley, C. W. & Denton, J. S., 2011, In : Frontiers in Pharmacology. 2 NOV, Article 75.

Research output: Contribution to journalArticle

28 Scopus citations

Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu4) with CNS exposure in rats

Engers, D. W., Field, J. R., Le, U., Zhou, Y., Bolinger, J. D., Zamorano, R., Blobaum, A. L., Jones, C. K., Jadhav, S., Weaver, C. D., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Feb 24 2011, In : Journal of Medicinal Chemistry. 54, 4, p. 1106-1110 5 p.

Research output: Contribution to journalArticle

33 Scopus citations

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

Jones, C. K., Engers, D. W., Thompson, A. D., Field, J. R., Blobaum, A. L., Lindsley, S. R., Zhou, Y., Gogliotti, R. D., Jadhav, S., Zamorano, R., Bogenpohl, J., Smith, Y., Morrison, R., Daniels, J. S., Weaver, C. D., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Nov 10 2011, In : Journal of Medicinal Chemistry. 54, 21, p. 7639-7647 9 p.

Research output: Contribution to journalArticle

46 Scopus citations

Discovery, synthesis, and structure-activity relationship of a series of N -aryl-bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a novel KCNQ2 and KCNQ4 potassium channel opener

Yu, H., Wu, M., Townsend, S. D., Zou, B., Long, S., Daniels, J. S., McManus, O. B., Li, M., Lindsley, C. W. & Hopkins, C. R., Oct 19 2011, In : ACS Chemical Neuroscience. 2, 10, p. 572-577 6 p.

Research output: Contribution to journalArticle

37 Scopus citations

Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels

Miller, M., Shi, J., Zhu, Y., Kustov, M., Tian, J. B., Stevens, A., Wu, M., Xu, J., Long, S., Yang, P., Zholos V, A., Salovich, J. M., Weaver, C. D., Hopkins, C. R., Lindsley, C. W., McManus, O., Li, M. & Zhu, M. X., Sep 23 2011, In : Journal of Biological Chemistry. 286, 38, p. 33436-33446 11 p.

Research output: Contribution to journalArticle

114 Scopus citations

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

Wood, M. R., Hopkins, C. R., Brogan, J. T., Conn, P. J. & Lindsley, C. W., Apr 5 2011, In : Biochemistry. 50, 13, p. 2403-2410 8 p.

Research output: Contribution to journalArticle

124 Scopus citations

Selective inhibition of the K ir2 family of inward rectifier potassium channels by a small molecule probe: The discovery, SAR, and pharmacological characterization of ML133

Wang, H. R., Wu, M., Yu, H., Long, S., Stevens, A., Engers, D. W., Sackin, H., Daniels, J. S., Dawson, E. S., Hopkins, C. R., Lindsley, C. W., Li, M. & McManus, O. B., Aug 19 2011, In : ACS chemical biology. 6, 8, p. 845-856 12 p.

Research output: Contribution to journalArticle

48 Scopus citations

Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu4

Cheung, Y. Y., Zamorano, R., Blobaum, A. L., Weaver, C. D., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Mar 14 2011, In : ACS Combinatorial Science. 13, 2, p. 159-165 7 p.

Research output: Contribution to journalArticle

4 Scopus citations

Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu 4) antagonist: Unexpected 'molecular switch' from a closely related mGlu 4 positive allosteric modulator

Utley, T., Haddenham, D., Salovich, J. M., Zamorano, R., Vinson, P. N., Lindsley, C. W., Hopkins, C. R. & Niswender, C. M., Dec 1 2011, In : Bioorganic and Medicinal Chemistry Letters. 21, 23, p. 6955-6959 5 p.

Research output: Contribution to journalArticle

15 Scopus citations

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

Xiang, Z., Thompson, A. D., Brogan, J. T., Schulte, M. L., Melancon, B. J., Mi, D., Lewis, L. M., Zou, B., Yang, L., Morrison, R., Santomango, T., Byers, F., Brewer, K., Aldrich, J. S., Yu, H., Dawson, E. S., Li, M., McManus, O., Jones, C. K., Daniels, J. S. & 5 others, Hopkins, C. R., Xie, X. S., Conn, P. J., Weaver, C. D. & Lindsley, C. W., Dec 21 2011, In : ACS Chemical Neuroscience. 2, 12, p. 730-742 13 p.

Research output: Contribution to journalArticle

47 Scopus citations
2010

ACS chemical neuroscience molecule spotlight on saphris

Hopkins, C. R., Apr 21 2010, In : ACS Chemical Neuroscience. 1, 4, p. 263-264 2 p.

Research output: Contribution to journalArticle

ACS chemical neuroscience molecule spotlight on valdoxen

Hopkins, C. R., Dec 15 2010, In : ACS Chemical Neuroscience. 1, 12, p. 772-773 2 p.

Research output: Contribution to journalArticle

1 Scopus citations

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M5 PAM

Bridges, T. M., Kennedy, J. P., Cho, H. P., Breininger, M. L., Gentry, P. R., Hopkins, C. R., Conn, P. J. & Lindsley, C. W., Jan 15 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 2, p. 558-562 5 p.

Research output: Contribution to journalArticle

35 Scopus citations

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

Bridges, T. M., Kennedy, J. P., Hopkins, C. R., Conn, P. J. & Lindsley, C. W., Oct 1 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 19, p. 5617-5622 6 p.

Research output: Contribution to journalArticle

22 Scopus citations

In vivo structure - Activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors

Hao, J., Ho, J. N., Lewis, J. A., Karim, K. A., Daniels, R. N., Gentry, P. R., Hopkins, C. R., Lindsley, C. W. & Hong, C. C., Feb 19 2010, In : ACS chemical biology. 5, 2, p. 245-253 9 p.

Research output: Contribution to journalArticle

239 Scopus citations

Re-exploration of the PHCCC scaffold: Discovery of improved positive allosteric modulators of mGluR4

Williams, R., Zhou, Y., Niswender, C. M., Luo, Q., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., Jun 16 2010, In : ACS Chemical Neuroscience. 1, 6, p. 411-419 9 p.

Research output: Contribution to journalArticle

40 Scopus citations

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu 4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Engers, D. W., Gentry, P. R., Williams, R., Bolinger, J. D., Weaver, C. D., Menon, U. N., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Sep 1 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 17, p. 5175-5178 4 p.

Research output: Contribution to journalArticle

20 Scopus citations

Synthesis of 1,3-diarylsubstituted indazoles utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence

Salovich, J. M., Lindsley, C. W. & Hopkins, C. R., Jul 21 2010, In : Tetrahedron Letters. 51, 29, p. 3796-3799 4 p.

Research output: Contribution to journalArticle

18 Scopus citations
2009

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

Engers, D. W., Niswender, C. M., Weaver, C. D., Jadhav, S., Menon, U. N., Zamorano, R., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., Jul 23 2009, In : Journal of Medicinal Chemistry. 52, 14, p. 4115-4118 4 p.

Research output: Contribution to journalArticle

61 Scopus citations

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

Williams, R., Johnson, K. A., Gentry, P. R., Niswender, C. M., Weaver, C. D., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., Sep 1 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 17, p. 4967-4970 4 p.

Research output: Contribution to journalArticle

25 Scopus citations
2006

Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-γ binding agents with potential application to the treatment of osteoporosis

Hopkins, C. R., O'Neil, S. V., Laufersweiler, M. C., Wang, Y., Pokross, M., Mekel, M., Evdokimov, A., Walter, R., Kontoyianni, M., Petrey, M. E., Sabatakos, G., Roesgen, J. T., Richardson, E. & Demuth, T. P., Nov 1 2006, In : Bioorganic and Medicinal Chemistry Letters. 16, 21, p. 5659-5663 5 p.

Research output: Contribution to journalArticle

37 Scopus citations

Development of N-4,6-pyrimidine-N-alkyl-N′-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase

Maier, J. A., Brugel, T. A., Sabat, M., Golebiowski, A., Laufersweiler, M. J., VanRens, J. C., Hopkins, C. R., De, B., Hsieh, L. C., Brown, K. K., Easwaran, V. & Janusz, M. J., Jul 15 2006, In : Bioorganic and Medicinal Chemistry Letters. 16, 14, p. 3646-3650 5 p.

Research output: Contribution to journalArticle

20 Scopus citations
2005

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase

Hopkins, C. R., Czekaj, M., Kaye, S. S., Gao, Z., Pribish, J., Pauls, H., Liang, G., Sides, K., Cramer, D., Cairns, J., Luo, Y., Lim, H. K., Vaz, R., Rebello, S., Maignan, S., Dupuy, A., Mathieu, M. & Levell, J., Jun 2 2005, In : Bioorganic and Medicinal Chemistry Letters. 15, 11, p. 2734-2737 4 p.

Research output: Contribution to journalArticle

29 Scopus citations

Synthesis of 6,7-disubstituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation

Hopkins, C. R. & Collar, N., Mar 14 2005, In : Tetrahedron Letters. 46, 11, p. 1845-1848 4 p.

Research output: Contribution to journalArticle

12 Scopus citations
2004
30 Scopus citations
25 Scopus citations

Convenient synthesis of 4-amino-3,5-disubstituted pyrazoles in one step from the corresponding diketo oximes

Majid, T., Hopkins, C. R., Pedgrift, B. & Collar, N., Mar 1 2004, In : Tetrahedron Letters. 45, 10, p. 2137-2139 3 p.

Research output: Contribution to journalArticle

23 Scopus citations

Novel pyrazinone inhibitors of mast cell tryptase: Synthesis and SAR evaluation

Hopkins, C., Neuenschwander, K., Scotese, A., Jackson, S., Nieduzak, T., Pauls, H., Liang, G., Sides, K., Cramer, D., Cairns, J., Maignan, S. & Mathieu, M., Oct 4 2004, In : Bioorganic and Medicinal Chemistry Letters. 14, 19, p. 4819-4823 5 p.

Research output: Contribution to journalArticle

28 Scopus citations
2002

Separation of Cdc25 dual specificity phosphatase inhibition and DNA cleaving activities in a focused library of analogs of the antitumor antibiotic Dnacin

Wipf, P., Hopkins, C. R., Phillips, E. O. & Lazo, J. S., Aug 5 2002, In : Tetrahedron. 58, 32, p. 6367-6372 6 p.

Research output: Contribution to journalArticle

17 Scopus citations
2001

Enantioselective synthesis of the AB-ring system of the antitumor antibiotic tetrazomine

Wipf, P. & Hopkins, C. R., May 4 2001, In : Journal of Organic Chemistry. 66, 9, p. 3133-3139 7 p.

Research output: Contribution to journalArticle

24 Scopus citations