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13 results

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Page 1
Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.
Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Bewley BR, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4274-4279. doi: 10.1016/j.bmcl.2017.08.043. Epub 2017 Aug 20. Bioorg Med Chem Lett. 2017. PMID: 28866269 Free PMC article.
VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.
Reed CW, McGowan KM, Spearing PK, Stansley BJ, Roenfanz HF, Engers DW, Rodriguez AL, Engelberg EM, Luscombe VB, Loch MT, Remke DH, Rook JM, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Reed CW, et al. Among authors: spearing pk. ACS Med Chem Lett. 2017 Nov 8;8(12):1326-1330. doi: 10.1021/acsmedchemlett.7b00429. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259756 Free PMC article.
Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.
Kalbfleisch JJ, Reed CW, Park C, Spearing PK, Quitalig MC, Jenkins MT, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Kalbfleisch JJ, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127529. doi: 10.1016/j.bmcl.2020.127529. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890686 Free PMC article.
Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes - Part 2.
Long MF, Capstick RA, Spearing PK, Engers JL, Gregro AR, Bollinger SR, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Lindsley CW, Engers DW, Temple KJ. Long MF, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2021 Dec 1;53:128416. doi: 10.1016/j.bmcl.2021.128416. Epub 2021 Oct 26. Bioorg Med Chem Lett. 2021. PMID: 34710625 Free PMC article.
Discovery of VU6024578/BI02982816: An mGlu1 Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models.
Reed CW, Kalbfleisch JF, Turkett JA, Trombley TA, Nastase AF, Spearing PK, Haymer DH, Sarwar MM, Quitalig M, Dickerson JW, Blobaum AL, Boutaud O, Voehringer P, Schuelert N, Cho HP, Niswender CM, Rook JM, Priepke H, Ursu D, Conn PJ, Melancon BJ, Lindsley CW. Reed CW, et al. Among authors: spearing pk. J Med Chem. 2024 Dec 26;67(24):22291-22312. doi: 10.1021/acs.jmedchem.4c02554. Epub 2024 Dec 12. J Med Chem. 2024. PMID: 39665415 Free PMC article.
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.
Henke BR, Consler TG, Go N, Hale RL, Hohman DR, Jones SA, Lu AT, Moore LB, Moore JT, Orband-Miller LA, Robinett RG, Shearin J, Spearing PK, Stewart EL, Turnbull PS, Weaver SL, Williams SP, Wisely GB, Lambert MH. Henke BR, et al. Among authors: spearing pk. J Med Chem. 2002 Dec 5;45(25):5492-505. doi: 10.1021/jm020291h. J Med Chem. 2002. PMID: 12459017
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.
Bass JY, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Mills WY, Navas F 3rd, Parks DJ, Smalley TL Jr, Spearing PK, Todd D, Williams SP, Wisely GB. Bass JY, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1206-13. doi: 10.1016/j.bmcl.2010.12.089. Epub 2010 Dec 23. Bioorg Med Chem Lett. 2011. PMID: 21256005
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.
Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Jones SA, Kaldor I, Liu Y, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F III, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB. Akwabi-Ameyaw A, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43. doi: 10.1016/j.bmcl.2008.06.073. Epub 2008 Jun 28. Bioorg Med Chem Lett. 2008. PMID: 18621523
13 results