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Three mechanistically distinct kinase assays compared: Measurement of intrinsic ATPase activity identified the most comprehensive set of ITK inhibitors.
Kashem MA, Nelson RM, Yingling JD, Pullen SS, Prokopowicz AS 3rd, Jones JW, Wolak JP, Rogers GR, Morelock MM, Snow RJ, Homon CA, Jakes S. Kashem MA, et al. Among authors: nelson rm. J Biomol Screen. 2007 Feb;12(1):70-83. doi: 10.1177/1087057106296047. Epub 2006 Dec 8. J Biomol Screen. 2007. PMID: 17166826
A high-throughput scintillation proximity assay for sphingosine-1-phosphate lyase.
Kashem MA, Wa C, Wolak JP, Grafos NS, Ryan KR, Sanville-Ross ML, Fogarty KE, Rybina IV, Shoultz A, Molinaro T, Desai SN, Rajan A, Huber JD, Nelson RM. Kashem MA, et al. Among authors: nelson rm. Assay Drug Dev Technol. 2014 Jun;12(5):293-302. doi: 10.1089/adt.2014.575. Epub 2014 May 20. Assay Drug Dev Technol. 2014. PMID: 24846303
A High-Throughput Genetic Complementation Assay in Yeast Cells Identified Selective Inhibitors of Sphingosine Kinase 1 Not Found Using a Cell-Free Enzyme Assay.
Kashem MA, Kennedy CA, Fogarty KE, Dimock JR, Zhang Y, Sanville-Ross ML, Skow DJ, Brunette SR, Swantek JL, Hummel HS, Swindle J, Nelson RM. Kashem MA, et al. Among authors: nelson rm. Assay Drug Dev Technol. 2016 Jan-Feb;14(1):39-49. doi: 10.1089/adt.2015.671. Epub 2015 Oct 1. Assay Drug Dev Technol. 2016. PMID: 26426296
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.
Wu JP, Fleck R, Brickwood J, Capolino A, Catron K, Chen Z, Cywin C, Emeigh J, Foerst M, Ginn J, Hrapchak M, Hickey E, Hao MH, Kashem M, Li J, Liu W, Morwick T, Nelson R, Marshall D, Martin L, Nemoto P, Potocki I, Liuzzi M, Peet GW, Scouten E, Stefany D, Turner M, Weldon S, Zimmitti C, Spero D, Kelly TA. Wu JP, et al. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5547-51. doi: 10.1016/j.bmcl.2009.08.054. Epub 2009 Aug 15. Bioorg Med Chem Lett. 2009. PMID: 19716697
Assay optimization: a statistical design of experiments approach.
Altekar M, Homon CA, Kashem MA, Mason SW, Nelson RM, Patnaude LA, Yingling J, Taylor PB. Altekar M, et al. Among authors: nelson rm. Clin Lab Med. 2007 Mar;27(1):139-54. doi: 10.1016/j.cll.2007.01.001. Clin Lab Med. 2007. PMID: 17416307
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Moss N, Breitfelder S, Betageri R, Cirillo PF, Fadra T, Hickey ER, Kirrane T, Kroe RR, Madwed J, Nelson RM, Pargellis CA, Qian KC, Regan J, Swinamer A, Torcellini C. Moss N, et al. Among authors: nelson rm. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4242-7. doi: 10.1016/j.bmcl.2007.05.042. Epub 2007 May 18. Bioorg Med Chem Lett. 2007. PMID: 17560108
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
Betageri R, Zhang Y, Zindell RM, Kuzmich D, Kirrane TM, Bentzien J, Cardozo M, Capolino AJ, Fadra TN, Nelson RM, Paw Z, Shih DT, Shih CK, Zuvela-Jelaska L, Nabozny G, Thomson DS. Betageri R, et al. Among authors: nelson rm. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4761-9. doi: 10.1016/j.bmcl.2005.07.025. Bioorg Med Chem Lett. 2005. PMID: 16112571
370 results