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Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Hudkins RL, Raddatz R, Tao M, Mathiasen JR, Aimone LD, Becknell NC, Prouty CP, Knutsen LJ, Yazdanian M, Moachon G, Ator MA, Mallamo JP, Marino MJ, Bacon ER, Williams M. Hudkins RL, et al. Among authors: williams m. J Med Chem. 2011 Jul 14;54(13):4781-92. doi: 10.1021/jm200401v. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634396
CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities.
Raddatz R, Hudkins RL, Mathiasen JR, Gruner JA, Flood DG, Aimone LD, Le S, Schaffhauser H, Duzic E, Gasior M, Bozyczko-Coyne D, Marino MJ, Ator MA, Bacon ER, Mallamo JP, Williams M. Raddatz R, et al. Among authors: williams m. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. doi: 10.1124/jpet.111.186585. Epub 2011 Oct 14. J Pharmacol Exp Ther. 2012. PMID: 22001260
3-(1'-Cyclobutylspiro[4H-1,3-benzodioxine-2,4'-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist.
Hudkins RL, Gruner JA, Raddatz R, Mathiasen JR, Aimone LD, Marino MJ, Bacon ER, Williams M, Ator MA. Hudkins RL, et al. Among authors: williams m. Neuropharmacology. 2016 Jul;106:37-45. doi: 10.1016/j.neuropharm.2015.09.025. Epub 2015 Sep 21. Neuropharmacology. 2016. PMID: 26400408
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
Dorsey BD, Iqbal M, Chatterjee S, Menta E, Bernardini R, Bernareggi A, Cassarà PG, D'Arasmo G, Ferretti E, De Munari S, Oliva A, Pezzoni G, Allievi C, Strepponi I, Ruggeri B, Ator MA, Williams M, Mallamo JP. Dorsey BD, et al. Among authors: williams m. J Med Chem. 2008 Feb 28;51(4):1068-72. doi: 10.1021/jm7010589. Epub 2008 Feb 5. J Med Chem. 2008. PMID: 18247547
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW. Rowbottom MW, et al. Among authors: williams m. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23. J Med Chem. 2012. PMID: 22168626
Receptors as drug targets.
Williams M, Raddatz R. Williams M, et al. Curr Protoc Pharmacol. 2006 Apr;Chapter 1:Unit 1.1. doi: 10.1002/0471141755.ph0101s32. Curr Protoc Pharmacol. 2006. PMID: 22294163
Overview of drug discovery and development.
Ator MA, Mallamo JP, Williams M. Ator MA, et al. Among authors: williams m. Curr Protoc Pharmacol. 2006 Dec;Chapter 9:Unit9.9. doi: 10.1002/0471141755.ph0909s35. Curr Protoc Pharmacol. 2006. PMID: 22294181
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.
Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J. Holladay MW, et al. Among authors: williams m. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21807507
CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.
James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW. James J, et al. Among authors: williams m. Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7. Mol Cancer Ther. 2012. PMID: 22319199
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