Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 64

1.

Selective allosteric modulation of muscarinic acetylcholine receptors for the treatment of schizophrenia and substance use disorders.

Teal LB, Gould RW, Felts AS, Jones CK.

Adv Pharmacol. 2019;86:153-196. doi: 10.1016/bs.apha.2019.05.001. Epub 2019 Jul 22.

PMID:
31378251
2.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, Daniels JS, Stec DF, Niswender CM, Jones CK, Wood MR, Wood MW, Duggan ME, Brandon NJ, Conn PJ, Bridges TM, Lindsley CW, Melancon BJ.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2224-2228. doi: 10.1016/j.bmcl.2019.06.032. Epub 2019 Jun 20.

PMID:
31248774
3.

VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.

Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, Brandon NJ, Dugan ME, Niswender CM, Jeffrey Conn P, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1714-1718. doi: 10.1016/j.bmcl.2019.05.026. Epub 2019 May 16.

PMID:
31113706
4.

Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.

Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

ACS Med Chem Lett. 2018 Oct 16;10(3):255-260. doi: 10.1021/acsmedchemlett.8b00426. eCollection 2019 Mar 14.

PMID:
30891122
5.

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.

Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):342-346. doi: 10.1016/j.bmcl.2018.10.050. Epub 2018 Nov 1.

PMID:
30503632
6.

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

Felts AS, Bollinger KA, Brassard CJ, Rodriguez AL, Morrison RD, Scott Daniels J, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Emmitte KA, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 1;29(1):47-50. doi: 10.1016/j.bmcl.2018.11.017. Epub 2018 Nov 10.

7.

Reducing Isolation and Loneliness Through Membership in a Fitness Program for Older Adults: Implications for Health.

Brady S, D'Ambrosio LA, Felts A, Rula EY, Kell KP, Coughlin JF.

J Appl Gerontol. 2020 Mar;39(3):301-310. doi: 10.1177/0733464818807820. Epub 2018 Nov 4.

PMID:
30392420
8.

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

J Med Chem. 2019 Jan 10;62(1):378-384. doi: 10.1021/acs.jmedchem.8b01266. Epub 2018 Oct 31.

PMID:
30350962
9.

Photoinduced Plasmon-Driven Chemistry in trans-1,2-Bis(4-pyridyl)ethylene Gold Nanosphere Oligomers.

Sprague-Klein EA, Negru B, Madison LR, Coste SC, Rugg BK, Felts AM, McAnally MO, Banik M, Apkarian VA, Wasielewski MR, Ratner MA, Seideman T, Schatz GC, Van Duyne RP.

J Am Chem Soc. 2018 Aug 22;140(33):10583-10592. doi: 10.1021/jacs.8b06347. Epub 2018 Aug 14.

PMID:
30071734
10.

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

Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1679-1685. doi: 10.1016/j.bmcl.2018.04.053. Epub 2018 Apr 22.

11.

Control of the Speed of a Light-Induced Spin Transition through Mesoscale Core-Shell Architecture.

Felts AC, Slimani A, Cain JM, Andrus MJ, Ahir AR, Abboud KA, Meisel MW, Boukheddaden K, Talham DR.

J Am Chem Soc. 2018 May 2;140(17):5814-5824. doi: 10.1021/jacs.8b02148. Epub 2018 Apr 20.

PMID:
29633838
12.

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.

O'Brien DE, Shaw DM, Cho HP, Cross AJ, Wesolowski SS, Felts AS, Bergare J, Elmore CS, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2018 May;93(5):526-540. doi: 10.1124/mol.117.110114. Epub 2018 Mar 15.

13.

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 AS, Rodriguez AL, Morrison RD, Bollinger KA, Venable DF, Blobaum AL, Byers FW, Thompson Gray A, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4858-4866. doi: 10.1016/j.bmcl.2017.09.042. Epub 2017 Sep 20.

14.

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

Bollinger KA, Felts AS, Brassard CJ, Engers JL, Rodriguez AL, Weiner RL, Cho HP, Chang S, Bubser M, Jones CK, Blobaum AL, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW.

ACS Med Chem Lett. 2017 Aug 3;8(9):919-924. doi: 10.1021/acsmedchemlett.7b00279. eCollection 2017 Sep 14.

15.

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).

Crouch RD, Blobaum AL, Felts AS, Conn PJ, Lindsley CW.

Drug Metab Dispos. 2017 Dec;45(12):1245-1259. doi: 10.1124/dmd.117.077552. Epub 2017 Sep 22.

PMID:
28939686
16.

Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.

Quadri M, Stokes C, Gulsevin A, Felts ACJ, Abboud KA, Papke RL, Horenstein NA.

J Med Chem. 2017 Sep 28;60(18):7928-7934. doi: 10.1021/acs.jmedchem.7b00875. Epub 2017 Sep 14.

17.

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 AS, Rodriguez AL, Blobaum AL, Morrison RD, Bates BS, Thompson Gray A, Rook JM, Tantawy MN, Byers FW, Chang S, Venable DF, Luscombe VB, Tamagnan GD, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

J Med Chem. 2017 Jun 22;60(12):5072-5085. doi: 10.1021/acs.jmedchem.7b00410. Epub 2017 May 31.

18.

Crystal structure of aqua-trans-bis-(dimethyl sulfoxide-κO)(pyridine-2,6-di-carboxyl-ato-κ3O2,N,O6)nickel(II).

Liu C, Felts AC, Takahashi D, Kinden WS, Abboud KA.

Acta Crystallogr E Crystallogr Commun. 2017 Apr 28;73(Pt 5):777-779. doi: 10.1107/S2056989017006090. eCollection 2017 May 1.

19.

Synergistic photomagnetic effects in coordination polymer heterostructure particles of Hofmann-like Fe(4-phenylpyridine)2[Ni(CN)4]·0.5H2O and K0.4Ni[Cr(CN)6]0.8·nH2O.

Gros CR, Peprah MK, Felts AC, Brinzari TV, Risset ON, Cain JM, Ferreira CF, Meisel MW, Talham DR.

Dalton Trans. 2016 Nov 14;45(42):16624-16634. Epub 2016 Aug 3.

PMID:
27484628
20.

Suicide in Elementary School-Aged Children and Early Adolescents.

Sheftall AH, Asti L, Horowitz LM, Felts A, Fontanella CA, Campo JV, Bridge JA.

Pediatrics. 2016 Oct;138(4). pii: e20160436. Epub 2016 Sep 19.

21.

Crystal structure of catena-poly[[(dimethyl sulfoxide-κO)(pyridine-2,6-di-carboxyl-ato-κ(3) O,N,O')nickel(II)]-μ-pyrazine-κ(2) N:N'].

Liu C, Thuijs AE, Felts AC, Ballouk HF, Abboud KA.

Acta Crystallogr E Crystallogr Commun. 2016 Apr 29;72(Pt 5):768-71. doi: 10.1107/S2056989016007064. eCollection 2016 May 1.

22.

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 AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1894-900. doi: 10.1016/j.bmcl.2016.03.026. Epub 2016 Mar 9.

23.

Crystal structure of catena-poly[[[trans-bis(aceto-nitrile-κN)diaquacobalt(II)]-μ-pyrazine-κ(2) N:N'] dinitrate].

Liu C, Felts AC, Thuijs AE, Useche A, Abboud KA.

Acta Crystallogr E Crystallogr Commun. 2016 Jan 13;72(Pt 2):151-4. doi: 10.1107/S2056989016000220. eCollection 2016 Feb 1.

24.

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

Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA.

J Med Chem. 2015 Nov 25;58(22):9027-40. doi: 10.1021/acs.jmedchem.5b01371. Epub 2015 Nov 11.

25.

Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects.

Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW, Jones CK.

Neuropsychopharmacology. 2016 Mar;41(4):1166-78. doi: 10.1038/npp.2015.265. Epub 2015 Aug 28.

26.

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

Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Neuropsychopharmacology. 2015 Feb;40(3):755-65. doi: 10.1038/npp.2014.245. Epub 2014 Sep 22.

27.

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

Bates BS, Rodriguez AL, Felts AS, Morrison RD, Venable DF, Blobaum AL, Byers FW, Lawson KP, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3307-14. doi: 10.1016/j.bmcl.2014.06.003. Epub 2014 Jun 11.

28.

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead.

Jones CK, Sheffler DJ, Williams R, Jadhav SB, Felts AS, Morrison RD, Niswender CM, Daniels JS, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1067-70. doi: 10.1016/j.bmcl.2014.01.013. Epub 2014 Jan 13.

29.

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

Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. doi: 10.1016/j.bmcl.2013.09.001. Epub 2013 Sep 10.

30.

Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway.

Theriault JR, Perez J, Gilbert S, Palmer M, Schreiber SL, Lindsley CW, Dawson ES, Engers JL, Felts AS, Bates BS, Emmitte KA.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 31 [updated 2013 Mar 14].

31.

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 KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17.

32.

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 CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, Daniels JS, Emmitte KA, Conn PJ, Lindsley CW.

J Med Chem. 2013 Jun 27;56(12):5208-12. doi: 10.1021/jm400439t. Epub 2013 Jun 13.

33.

The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor.

Blobaum AL, Uddin MJ, Felts AS, Crews BC, Rouzer CA, Marnett LJ.

ACS Med Chem Lett. 2013 May 9;4(5):486-490. Epub 2013 Mar 25.

34.

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 RJ, Felts AS, Rodriguez AL, Venable DF, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Emmitte KA.

ACS Chem Neurosci. 2013 Aug 21;4(8):1217-28. doi: 10.1021/cn400070k. Epub 2013 May 29.

35.

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

Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2012 Nov;82(5):860-75. doi: 10.1124/mol.112.080531. Epub 2012 Aug 3.

36.

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

Morrison RD, Blobaum AL, Byers FW, Santomango TS, Bridges TM, Stec D, Brewer KA, Sanchez-Ponce R, Corlew MM, Rush R, Felts AS, Manka J, Bates BS, Venable DF, Rodriguez AL, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA, Daniels JS.

Drug Metab Dispos. 2012 Sep;40(9):1834-45. doi: 10.1124/dmd.112.046136. Epub 2012 Jun 18.

37.

Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.

Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, Olsen CM, Winder DG, Emmitte KA, Lindsley CW.

ChemMedChem. 2012 Mar 5;7(3):406-14. doi: 10.1002/cmdc.201100510. Epub 2012 Jan 20. No abstract available.

38.

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

Theriault JR, Felts AS, Bates BS, Perez JR, Palmer M, Gilbert SR, Dawson ES, Engers JL, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81. doi: 10.1016/j.bmcl.2011.11.077. Epub 2011 Nov 28.

39.

Identification of alternative binding sites for inhibitors of HIV-1 ribonuclease H through comparative analysis of virtual enrichment studies.

Felts AK, Labarge K, Bauman JD, Patel DV, Himmel DM, Arnold E, Parniak MA, Levy RM.

J Chem Inf Model. 2011 Aug 22;51(8):1986-98. doi: 10.1021/ci200194w. Epub 2011 Jul 26.

40.

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 AS, Lindsley SR, Lamb JP, Rodriguez AL, Menon UN, Jadhav S, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. doi: 10.1016/j.bmcl.2010.06.064. Epub 2010 Jun 15.

41.

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. doi: 10.1016/j.bmcl.2009.10.024. Epub 2009 Oct 9.

43.

The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives.

Walters MJ, Blobaum AL, Kingsley PJ, Felts AS, Sulikowski GA, Marnett LJ.

Bioorg Med Chem Lett. 2009 Jun 15;19(12):3271-4. doi: 10.1016/j.bmcl.2009.04.078. Epub 2009 Apr 23.

45.

Prediction of Protein Loop Conformations using the AGBNP Implicit Solvent Model and Torsion Angle Sampling.

Felts AK, Gallicchio E, Chekmarev D, Paris KA, Friesner RA, Levy RM.

J Chem Theory Comput. 2008;4(5):855-868.

46.

Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition.

Felts AS, Siegel BS, Young SM, Moth CW, Lybrand TP, Dannenberg AJ, Marnett LJ, Subbaramaiah K.

J Med Chem. 2008 Aug 28;51(16):4911-9. doi: 10.1021/jm700969c. Epub 2008 Jul 30.

47.

Desmethyl derivatives of indomethacin and sulindac as probes for cyclooxygenase-dependent biology.

Felts AS, Ji C, Stafford JB, Crews BC, Kingsley PJ, Rouzer CA, Washington MK, Subbaramaiah K, Siegel BS, Young SM, Dannenberg AJ, Marnett LJ.

ACS Chem Biol. 2007 Jul 20;2(7):479-83. Epub 2007 Jun 29.

PMID:
17602619
48.
49.

Distinguishing among structural ensembles of the GB1 peptide: REMD simulations and NMR experiments.

Weinstock DS, Narayanan C, Felts AK, Andrec M, Levy RM, Wu KP, Baum J.

J Am Chem Soc. 2007 Apr 25;129(16):4858-9. Epub 2007 Apr 3. No abstract available.

50.

Temperature weighted histogram analysis method, replica exchange, and transition paths.

Gallicchio E, Andrec M, Felts AK, Levy RM.

J Phys Chem B. 2005 Apr 14;109(14):6722-31.

PMID:
16851756

Supplemental Content

Support Center