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Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui CE, Deng N, Ferguson AD, Kawatkar S, Grimster NP, Ruston L, Lyne PD, Read JA, Peng X, Pei X, Fawell S, Tang Z, Throner S, Vasbinder MM, Wang H, Winter-Holt J, Woessner R, Wu A, Yang W, Zinda M, Kettle JG. Su Q, et al. Among authors: kawatkar s. J Med Chem. 2020 May 14;63(9):4517-4527. doi: 10.1021/acs.jmedchem.9b01392. Epub 2020 Apr 28. J Med Chem. 2020. PMID: 32297743
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).
Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA. Martínez-Botella G, et al. Among authors: kawatkar s. J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23043329
Identification of azabenzimidazoles as potent JAK1 selective inhibitors.
Vasbinder MM, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Goodwin K, Huszar D, Kawatkar A, Kawatkar S, Read J, Shi J, Steinbacher S, Steuber H, Su Q, Toader D, Wang H, Woessner R, Wu A, Ye M, Zinda M. Vasbinder MM, et al. Among authors: kawatkar a, kawatkar s. Bioorg Med Chem Lett. 2016 Jan 1;26(1):60-7. doi: 10.1016/j.bmcl.2015.11.031. Epub 2015 Nov 12. Bioorg Med Chem Lett. 2016. PMID: 26614408
Rapid Identification of Novel Allosteric PRC2 Inhibitors.
Read JA, Tart J, Rawlins PB, Gregson C, Jones K, Gao N, Zhu X, Tomlinson R, Code E, Cheung T, Chen H, Kawatkar SP, Bloecher A, Bagal S, O'Donovan DH, Robinson J. Read JA, et al. Among authors: kawatkar sp. ACS Chem Biol. 2019 Oct 18;14(10):2134-2140. doi: 10.1021/acschembio.9b00468. Epub 2019 Sep 23. ACS Chem Biol. 2019. PMID: 31525019
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex.
Hsu JH, Rasmusson T, Robinson J, Pachl F, Read J, Kawatkar S, O' Donovan DH, Bagal S, Code E, Rawlins P, Argyrou A, Tomlinson R, Gao N, Zhu X, Chiarparin E, Jacques K, Shen M, Woods H, Bednarski E, Wilson DM, Drew L, Castaldi MP, Fawell S, Bloecher A. Hsu JH, et al. Among authors: kawatkar s. Cell Chem Biol. 2020 Jan 16;27(1):41-46.e17. doi: 10.1016/j.chembiol.2019.11.004. Epub 2019 Nov 27. Cell Chem Biol. 2020. PMID: 31786184 Free article.
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: kawatkar s. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.
Kawatkar SP, Barlaam B, Kemmitt P, Simpson I, Watson D, Wang P, Lamont S, Su Q, Boiko S, Ikeda T, Patel J, Pike A, Pollard H, Read J, Sarkar U, Wang H, Wen Q, Yan Z, Dowling JE, Dry H, Edmondson SD. Kawatkar SP, et al. Bioorg Med Chem Lett. 2020 Sep 15;30(18):127393. doi: 10.1016/j.bmcl.2020.127393. Epub 2020 Jul 10. Bioorg Med Chem Lett. 2020. PMID: 32721854
Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.
Barlaam B, Boiko S, Boyd S, Dry H, Gingipalli L, Ikeda T, Johnson T, Kawatkar S, Lorthioir O, Pike A, Pollard H, Read J, Su Q, Wang H, Wang H, Wang L, Wang P, Edmondson SD. Barlaam B, et al. Among authors: kawatkar s. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127523. doi: 10.1016/j.bmcl.2020.127523. Epub 2020 Aug 30. Bioorg Med Chem Lett. 2020. PMID: 32877741
27 results