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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14.
J Med Chem. 2017.
PMID: 28498658
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR.
Gerstenberger BS, et al. Among authors: samardjiev ij.
J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3.
J Med Chem. 2016.
PMID: 27115555
Free PMC article.
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2,6-Diisopropyl-anilinium chloride.
Samardjiev I, Samas B.
Samardjiev I, et al.
Acta Crystallogr Sect E Struct Rep Online. 2008 Jul 12;64(Pt 8):o1480. doi: 10.1107/S160053680801790X.
Acta Crystallogr Sect E Struct Rep Online. 2008.
PMID: 21203192
Free PMC article.
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An asymmetric synthesis of (2S,5S)-5-substituted azepane-2-carboxylate derivatives.
Wishka DG, Bédard M, Brighty KE, Buzon RA, Farley KA, Fichtner MW, Kauffman GS, Kooistra J, Lewis JG, O'Dowd H, Samardjiev IJ, Samas B, Yalamanchi G, Noe MC.
Wishka DG, et al. Among authors: samardjiev ij.
J Org Chem. 2011 Mar 18;76(6):1937-40. doi: 10.1021/jo102475s. Epub 2011 Jan 28.
J Org Chem. 2011.
PMID: 21275376
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The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
Le PT, Brickner SJ, Wade SK, Brighty K, Monahan R, Stone GG, Girard D, Finegan S, Duignan J, Schafer J, Maloney M, Zaniewski RP, Connolly AG, Liras J, Bordner J, Samardjiev I.
Le PT, et al.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):276-9. doi: 10.1016/j.bmcl.2010.11.022. Epub 2010 Nov 10.
Bioorg Med Chem Lett. 2011.
PMID: 21115249
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Molecular features crucial to the activity of pyrimidine benzamide-based thrombopoietin receptor agonists.
Reiter LA, Jones CS, Brissette WH, McCurdy SP, Abramov YA, Bordner J, DiCapua FM, Munchhof MJ, Rescek DM, Samardjiev IJ, Withka JM.
Reiter LA, et al. Among authors: samardjiev ij.
Bioorg Med Chem Lett. 2008 May 1;18(9):3000-6. doi: 10.1016/j.bmcl.2008.03.052. Epub 2008 Mar 20.
Bioorg Med Chem Lett. 2008.
PMID: 18396041
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Twisted amide reduction under Wolff-Kishner conditions: synthesis of a benzo-1-aza-adamantane derivative.
Bashore CG, Samardjiev IJ, Bordner J, Coe JW.
Bashore CG, et al. Among authors: samardjiev ij.
J Am Chem Soc. 2003 Mar 19;125(11):3268-72. doi: 10.1021/ja028152c.
J Am Chem Soc. 2003.
PMID: 12630882
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Solid-state characterization of an NR2B selective N-methyl d-aspartate (NMDA) antagonist polymorphs.
Kojima T, Sato M, Omura A, Kawai M, Sakai M, Matsuoka Y, Murata Y, Hattori K, Sakemi S, Bordner J, Samardjiev I, Mano T.
Kojima T, et al.
Int J Pharm. 2008 May 1;355(1-2):337-40. doi: 10.1016/j.ijpharm.2007.11.060. Epub 2007 Dec 7.
Int J Pharm. 2008.
PMID: 18242021
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