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Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106.
Heinrich T, Peterson C, Schneider R, Garg S, Schwarz D, Gunera J, Seshire A, Kötzner L, Schlesiger S, Musil D, Schilke H, Doerfel B, Diehl P, Böpple P, Lemos AR, Sousa PMF, Freire F, Bandeiras TM, Carswell E, Pearson N, Sirohi S, Hooker M, Trivier E, Broome R, Balsiger A, Crowden A, Dillon C, Wienke D. Heinrich T, et al. Among authors: carswell e. J Med Chem. 2022 Jul 14;65(13):9206-9229. doi: 10.1021/acs.jmedchem.2c00403. Epub 2022 Jun 28. J Med Chem. 2022. PMID: 35763499
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Hoyt SB, Park MK, London C, Xiong Y, Tata J, Bennett DJ, Cooke A, Cai J, Carswell E, Robinson J, MacLean J, Brown L, Belshaw S, Clarkson TR, Liu K, Liang GB, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Kuethe J, Rivera N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Ali A. Hoyt SB, et al. Among authors: carswell e. ACS Med Chem Lett. 2015 Apr 7;6(5):573-8. doi: 10.1021/acsmedchemlett.5b00054. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005536 Free PMC article.
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Hussain Z, Cooke AJ, Neelamkavil S, Brown L, Carswell E, Geissler WM, Guo Z, Hawes B, Kelly TM, Kiyoi Y, Lai K, Lesburg C, Pow E, Zang Y, Wood HB, Edmondson SD, Liu W. Hussain Z, et al. Among authors: carswell e. Bioorg Med Chem Lett. 2020 Aug 15;30(16):127072. doi: 10.1016/j.bmcl.2020.127072. Epub 2020 Feb 29. Bioorg Med Chem Lett. 2020. PMID: 32340773
Imidazopyridyl compounds as aldosterone synthase inhibitors.
Whitehead BR, Lo MM, Ali A, Park MK, Hoyt SB, Xiong Y, Cai J, Carswell E, Cooke A, MacLean J, Ratcliffe P, Robinson J, Bennett DJ, Clemas JA, Wisniewski T, Struthers M, Cully D, MacNeil DJ. Whitehead BR, et al. Among authors: carswell e. Bioorg Med Chem Lett. 2017 Jan 15;27(2):143-146. doi: 10.1016/j.bmcl.2016.12.003. Epub 2016 Dec 2. Bioorg Med Chem Lett. 2017. PMID: 27979595
High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.
Fradera X, Kazemier B, Carswell E, Cooke A, Oubrie A, Hamilton W, Dempster M, Krapp S, Nagel S, Jestel A. Fradera X, et al. Among authors: carswell e. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Apr 1;68(Pt 4):404-8. doi: 10.1107/S1744309112009037. Epub 2012 Mar 27. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012. PMID: 22505407 Free PMC article.
Si-free enolate Claisen rearrangements of enamido substrates.
Harker WR, Carswell EL, Carbery DR. Harker WR, et al. Among authors: carswell el. Org Biomol Chem. 2012 Feb 21;10(7):1406-10. doi: 10.1039/c2ob06853b. Epub 2012 Jan 4. Org Biomol Chem. 2012. PMID: 22215234 Free article.
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