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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: embrey k. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW. Tron AE, et al. Among authors: embrey kj. Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w. Nat Commun. 2018. PMID: 30559424 Free PMC article.
MTH1 Substrate Recognition--An Example of Specific Promiscuity.
Nissink JW, Bista M, Breed J, Carter N, Embrey K, Read J, Winter-Holt JJ. Nissink JW, et al. Among authors: embrey k. PLoS One. 2016 Mar 21;11(3):e0151154. doi: 10.1371/journal.pone.0151154. eCollection 2016. PLoS One. 2016. PMID: 26999531 Free PMC article.
Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors.
Naik M, Raichurkar A, Bandodkar BS, Varun BV, Bhat S, Kalkhambkar R, Murugan K, Menon R, Bhat J, Paul B, Iyer H, Hussein S, Tucker JA, Vogtherr M, Embrey KJ, McMiken H, Prasad S, Gill A, Ugarkar BG, Venkatraman J, Read J, Panda M. Naik M, et al. Among authors: embrey kj. J Med Chem. 2015 Jan 22;58(2):753-66. doi: 10.1021/jm5012947. Epub 2014 Dec 23. J Med Chem. 2015. PMID: 25486447
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Collie GW, Michaelides IN, Embrey K, Stubbs CJ, Börjesson U, Dale IL, Snijder A, Barlind L, Song K, Khurana P, Phillips C, Storer RI. Collie GW, et al. Among authors: embrey k. ACS Med Chem Lett. 2020 Dec 8;12(1):162-167. doi: 10.1021/acsmedchemlett.0c00392. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488978 Free PMC article.
Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation.
Winter JJ, Anderson M, Blades K, Brassington C, Breeze AL, Chresta C, Embrey K, Fairley G, Faulder P, Finlay MR, Kettle JG, Nowak T, Overman R, Patel SJ, Perkins P, Spadola L, Tart J, Tucker JA, Wrigley G. Winter JJ, et al. Among authors: embrey k. J Med Chem. 2015 Mar 12;58(5):2265-74. doi: 10.1021/jm501660t. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25695162 Free article.
Structure-based design of protein tyrosine phosphatase-1B inhibitors.
Black E, Breed J, Breeze AL, Embrey K, Garcia R, Gero TW, Godfrey L, Kenny PW, Morley AD, Minshull CA, Pannifer AD, Read J, Rees A, Russell DJ, Toader D, Tucker J. Black E, et al. Among authors: embrey k. Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7. doi: 10.1016/j.bmcl.2005.03.068. Bioorg Med Chem Lett. 2005. PMID: 15863305
34 results