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Page 1
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
Butler CR, Popiolek M, McAllister LA, LaChapelle EA, Kramer M, Beck EM, Mente S, Brodney MA, Brown M, Gilbert A, Helal C, Ogilvie K, Starr J, Uccello D, Grimwood S, Edgerton J, Garst-Orozco J, Kozak R, Lotarski S, Rossi A, Smith D, O'Connor R, Lazzaro J, Steppan C, Steyn SJ. Butler CR, et al. Among authors: gilbert a. J Med Chem. 2024 Jul 11;67(13):10831-10847. doi: 10.1021/acs.jmedchem.4c00293. Epub 2024 Jun 18. J Med Chem. 2024. PMID: 38888621
1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.
Piatnitski Chekler EL, Unwalla R, Khan TA, Tangirala RS, Johnson M, St Andre M, Anderson JT, Kenney T, Chiparri S, McNally C, Kilbourne E, Thompson C, Nagpal S, Weber G, Schelling S, Owens J, Morris CA, Powell D, Verhoest PR, Gilbert AM. Piatnitski Chekler EL, et al. Among authors: gilbert am. J Med Chem. 2014 Mar 27;57(6):2462-71. doi: 10.1021/jm401625b. Epub 2014 Mar 10. J Med Chem. 2014. PMID: 24527807
Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors.
Flanagan ME, Abramite JA, Anderson DP, Aulabaugh A, Dahal UP, Gilbert AM, Li C, Montgomery J, Oppenheimer SR, Ryder T, Schuff BP, Uccello DP, Walker GS, Wu Y, Brown MF, Chen JM, Hayward MM, Noe MC, Obach RS, Philippe L, Shanmugasundaram V, Shapiro MJ, Starr J, Stroh J, Che Y. Flanagan ME, et al. Among authors: gilbert am. J Med Chem. 2014 Dec 11;57(23):10072-9. doi: 10.1021/jm501412a. Epub 2014 Nov 26. J Med Chem. 2014. PMID: 25375838
Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.
Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM. Huard K, et al. Among authors: gilbert a. J Med Chem. 2016 Feb 11;59(3):1165-75. doi: 10.1021/acs.jmedchem.5b01752. Epub 2016 Jan 27. J Med Chem. 2016. PMID: 26734723
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Ahn K, Boehm M, Brown MF, Calloway J, Che Y, Chen J, Fennell KF, Geoghegan KF, Gilbert AM, Gutierrez JA, Kalgutkar AS, Lanba A, Limberakis C, Magee TV, O'Doherty I, Oliver R, Pabst B, Pandit J, Parris K, Pfefferkorn JA, Rolph TP, Patel R, Schuff B, Shanmugasundaram V, Starr JT, Varghese AH, Vera NB, Vernochet C, Yan J. Ahn K, et al. Among authors: gilbert am. ACS Chem Biol. 2016 Sep 16;11(9):2529-40. doi: 10.1021/acschembio.6b00266. Epub 2016 Jul 19. ACS Chem Biol. 2016. PMID: 27391855
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.
Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB. Thorarensen A, et al. Among authors: gilbert am. J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16. J Med Chem. 2017. PMID: 28139931
Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.
Unwalla R, Mousseau JJ, Fadeyi OO, Choi C, Parris K, Hu B, Kenney T, Chippari S, McNally C, Vishwanathan K, Kilbourne E, Thompson C, Nagpal S, Wrobel J, Yudt M, Morris CA, Powell D, Gilbert AM, Chekler ELP. Unwalla R, et al. Among authors: gilbert am. J Med Chem. 2017 Jul 27;60(14):6451-6457. doi: 10.1021/acs.jmedchem.7b00373. Epub 2017 Jul 11. J Med Chem. 2017. PMID: 28696695
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
McAllister LA, Butler CR, Mente S, O'Neil SV, Fonseca KR, Piro JR, Cianfrogna JA, Foley TL, Gilbert AM, Harris AR, Helal CJ, Johnson DS, Montgomery JI, Nason DM, Noell S, Pandit J, Rogers BN, Samad TA, Shaffer CL, da Silva RG, Uccello DP, Webb D, Brodney MA. McAllister LA, et al. Among authors: gilbert am. J Med Chem. 2018 Apr 12;61(7):3008-3026. doi: 10.1021/acs.jmedchem.8b00070. Epub 2018 Mar 15. J Med Chem. 2018. PMID: 29498843
Delineating the role of cooperativity in the design of potent PROTACs for BTK.
Zorba A, Nguyen C, Xu Y, Starr J, Borzilleri K, Smith J, Zhu H, Farley KA, Ding W, Schiemer J, Feng X, Chang JS, Uccello DP, Young JA, Garcia-Irrizary CN, Czabaniuk L, Schuff B, Oliver R, Montgomery J, Hayward MM, Coe J, Chen J, Niosi M, Luthra S, Shah JC, El-Kattan A, Qiu X, West GM, Noe MC, Shanmugasundaram V, Gilbert AM, Brown MF, Calabrese MF. Zorba A, et al. Among authors: gilbert am. Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):E7285-E7292. doi: 10.1073/pnas.1803662115. Epub 2018 Jul 16. Proc Natl Acad Sci U S A. 2018. PMID: 30012605 Free PMC article.
1,759 results