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134,995 results

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Page 1
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Koester DC, Marx VM, Williams S, Jiricek J, Dauphinais M, René O, Miller SL, Zhang L, Patra D, Chen YL, Cheung H, Gable J, Lakshminarayana SB, Osborne C, Galarneau JR, Kulkarni U, Richmond W, Bretz A, Xiao L, Supek F, Wiesmann C, Honnappa S, Be C, Mäser P, Kaiser M, Ritchie R, Barrett MP, Diagana TT, Sarko C, Rao SPS. Koester DC, et al. Among authors: zhang l. J Med Chem. 2022 Sep 8;65(17):11776-11787. doi: 10.1021/acs.jmedchem.2c00791. Epub 2022 Aug 22. J Med Chem. 2022. PMID: 35993839 Free PMC article.
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL. Zhang L, et al. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.
Davoren JE, Garnsey M, Pettersen B, Brodney MA, Edgerton JR, Fortin JP, Grimwood S, Harris AR, Jenkinson S, Kenakin T, Lazzaro JT, Lee CW, Lotarski SM, Nottebaum L, O'Neil SV, Popiolek M, Ramsey S, Steyn SJ, Thorn CA, Zhang L, Webb D. Davoren JE, et al. Among authors: zhang l. J Med Chem. 2017 Aug 10;60(15):6649-6663. doi: 10.1021/acs.jmedchem.7b00597. Epub 2017 Jul 26. J Med Chem. 2017. PMID: 28598634
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Ghosh S, Hou X, Houle C, Karki K, Lazzaro JT, Mancuso JY, Marcek JM, Miller EL, Moen MA, O'Neil S, Sakurada I, Skaddan M, Parikh V, Smith DL, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Won A, Wright AS, Whritenour J, Zasadny K, Zaleska MM, Zhang L, Shaffer CL. Stepan AF, et al. Among authors: zhang l. J Med Chem. 2017 Sep 28;60(18):7764-7780. doi: 10.1021/acs.jmedchem.7b00604. Epub 2017 Sep 13. J Med Chem. 2017. PMID: 28817277
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Ma B, Bohnert T, Otipoby KL, Tien E, Arefayene M, Bai J, Bajrami B, Bame E, Chan TR, Humora M, MacPhee JM, Marcotte D, Mehta D, Metrick CM, Moniz G, Polack E, Poreci U, Prefontaine A, Sheikh S, Schroeder P, Smirnakis K, Zhang L, Zheng F, Hopkins BT. Ma B, et al. Among authors: zhang l. J Med Chem. 2020 Nov 12;63(21):12526-12541. doi: 10.1021/acs.jmedchem.0c00702. Epub 2020 Aug 6. J Med Chem. 2020. PMID: 32696648
Discovery of Potent Selective Nonzinc Binding Autotaxin Inhibitor BIO-32546.
Ma B, Zhang L, Sun L, Xin Z, Kumaravel G, Marcotte D, Chodaparambil JV, Wang Q, Wehr A, Jing J, Hong VS, Wang T, Huang C, Shao Z, Mi S. Ma B, et al. Among authors: zhang l. ACS Med Chem Lett. 2021 Jun 14;12(7):1124-1129. doi: 10.1021/acsmedchemlett.1c00211. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267882 Free PMC article.
Identification of Potent, Broad-Spectrum Coronavirus Main Protease Inhibitors for Pandemic Preparedness.
Barkan DT, Garland K, Zhang L, Eastman RT, Hesse M, Knapp M, Ornelas E, Tang J, Cortopassi WA, Wang Y, King F, Jia W, Nguyen Z, Frank AO, Chan R, Fang E, Fuller D, Busby S, Carias H, Donahue K, Tandeske L, Diagana TT, Jarrousse N, Moser H, Sarko C, Dovala D, Moquin S, Marx VM. Barkan DT, et al. Among authors: zhang l. J Med Chem. 2024 Oct 10;67(19):17454-17471. doi: 10.1021/acs.jmedchem.4c01404. Epub 2024 Sep 27. J Med Chem. 2024. PMID: 39332817 Free PMC article.
Discovery of PF-07265028, A Selective Small Molecule Inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1) for the Treatment of Cancer.
Gallego RA, Cho-Schultz S, Del Bel M, Dechert-Schmitt AM, Donaldson JS, He M, Jalaie M, Kania R, Matthews J, McTigue M, Tuttle JB, Risley H, Zhou D, Zhou R, Ahmad OK, Bernier L, Berritt S, Braganza J, Chen Z, Cianfrogna JA, Collins M, Costa Jones C, Cronin CN, Davis C, Dress K, Edwards M, Farrell W, France SP, Grable N, Johnson E, Johnson TW, Jones R, Knauber T, Lafontaine J, Loach RP, Maestre M, Miller N, Moen M, Monfette S, Morse P, Nager AR, Niosi M, Richardson P, Rohner AK, Sach NW, Timofeevski S, Tucker JW, Vetelino B, Zhang L, Nair SK. Gallego RA, et al. Among authors: zhang l. J Med Chem. 2024 Dec 26;67(24):22002-22038. doi: 10.1021/acs.jmedchem.4c01930. Epub 2024 Dec 9. J Med Chem. 2024. PMID: 39651809 Clinical Trial.
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.
Duplantier AJ, Becker SL, Bohanon MJ, Borzilleri KA, Chrunyk BA, Downs JT, Hu LY, El-Kattan A, James LC, Liu S, Lu J, Maklad N, Mansour MN, Mente S, Piotrowski MA, Sakya SM, Sheehan S, Steyn SJ, Strick CA, Williams VA, Zhang L. Duplantier AJ, et al. Among authors: zhang l. J Med Chem. 2009 Jun 11;52(11):3576-85. doi: 10.1021/jm900128w. J Med Chem. 2009. PMID: 19438227
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