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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: helal c. 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
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. 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
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.
Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S. Davoren JE, et al. Among authors: helal cj. J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27275946
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. J Med Chem. 2017. PMID: 28574706
The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.
Zhang L, Chen L, Beck EM, Chappie TA, Coelho RV, Doran SD, Fan KH, Helal CJ, Humphrey JM, Hughes Z, Kuszpit K, Lachapelle EA, Lazzaro JT, Lee C, Mather RJ, Patel NC, Skaddan MB, Sciabola S, Verhoest PR, Young JM, Zasadny K, Villalobos A. Zhang L, et al. Among authors: helal cj. J Med Chem. 2017 Oct 26;60(20):8538-8551. doi: 10.1021/acs.jmedchem.7b01050. Epub 2017 Oct 9. J Med Chem. 2017. PMID: 28957634
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.
Davoren JE, Nason D, Coe J, Dlugolenski K, Helal C, Harris AR, LaChapelle E, Liang S, Liu Y, O'Connor R, Orozco CC, Rai BK, Salafia M, Samas B, Xu W, Kozak R, Gray D. Davoren JE, et al. Among authors: helal c. J Med Chem. 2018 Dec 27;61(24):11384-11397. doi: 10.1021/acs.jmedchem.8b01622. Epub 2018 Dec 11. J Med Chem. 2018. PMID: 30431269
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Butler TW, Dorff PH, Efremov IV, Evrard E, Green ME, Helal CJ, Kauffman GW, Mullins PB, Navaratnam T, O'Donnell CJ, O'Sullivan TJ, Patel NC, Stepan AF, Stiff CM, Subramanyam C, Trapa P, Tran TP, Vetelino BC, Yang E, Xie L, Pustilnik LR, Steyn SJ, Wood KM, Bales KR, Hajos-Korcsok E, Verhoest PR. Pettersson M, et al. Among authors: helal cj. J Med Chem. 2024 Jun 27;67(12):10248-10262. doi: 10.1021/acs.jmedchem.4c00580. Epub 2024 Jun 7. J Med Chem. 2024. PMID: 38848667
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.
Zhang L, Villalobos A, Beck EM, Bocan T, Chappie TA, Chen L, Grimwood S, Heck SD, Helal CJ, Hou X, Humphrey JM, Lu J, Skaddan MB, McCarthy TJ, Verhoest PR, Wager TT, Zasadny K. Zhang L, et al. J Med Chem. 2013 Jun 13;56(11):4568-79. doi: 10.1021/jm400312y. Epub 2013 May 28. J Med Chem. 2013. PMID: 23651455
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.
Butler CR, Ogilvie K, Martinez-Alsina L, Barreiro G, Beck EM, Nolan CE, Atchison K, Benvenuti E, Buzon L, Doran S, Gonzales C, Helal CJ, Hou X, Hsu MH, Johnson EF, Lapham K, Lanyon L, Parris K, O'Neill BT, Riddell D, Robshaw A, Vajdos F, Brodney MA. Butler CR, et al. Among authors: helal cj. J Med Chem. 2017 Jan 12;60(1):386-402. doi: 10.1021/acs.jmedchem.6b01451. Epub 2016 Dec 20. J Med Chem. 2017. PMID: 27997172 Free PMC article.
44 results