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Page 1
Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Bennett J, Boucharens S, Black D, Cook A, Brown AR, Epemolu O, Fletcher D, Haunso A, Huggett M, Jones P, Laats S, Lyons A, Mestres J, de Man J, Morphy R, Rankovic Z, Sherborne B, Sherry L, van Straten N, Westwood P, Zaman GZ. Ray P, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Jan 1;21(1):97-101. doi: 10.1016/j.bmcl.2010.11.060. Epub 2010 Nov 19. Bioorg Med Chem Lett. 2011. PMID: 21145740
The first potent and selective inhibitors of the glycine transporter type 2.
Caulfield WL, Collie IT, Dickins RS, Epemolu O, McGuire R, Hill DR, McVey G, Morphy JR, Rankovic Z, Sundaram H. Caulfield WL, et al. Among authors: epemolu o. J Med Chem. 2001 Aug 16;44(17):2679-82. doi: 10.1021/jm0011272. J Med Chem. 2001. PMID: 11495577 No abstract available.
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Reid M, Carlyle I, Caulfield WL, Clarkson TR, Cusick F, Epemolu O, Gilfillan R, Goodwin R, Jaap D, O'Donnell EC, Presland J, Rankovic Z, Spinks D, Spinks G, Thomson AM, Thomson F, Strain J, Wishart G. Reid M, et al. Among authors: o donnell ec, epemolu o. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3713-6. doi: 10.1016/j.bmcl.2010.04.085. Epub 2010 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20471831
Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M. Ray P, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1084-8. doi: 10.1016/j.bmcl.2010.12.104. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21251828
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, Feilden H, Fields R, Francis S, Jeremiah F, McArthur D, Morrison AJ, Prosser A, Ratcliffe PD, Schulz J, Wishart G, Baker J, Campbell R, Cottney JE, Deehan M, Epemolu O, Evans L. Kiyoi T, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1748-53. doi: 10.1016/j.bmcl.2011.01.082. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316962
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.
Ratcliffe P, Adam JM, Baker J, Bursi R, Campbell R, Clark JK, Cottney JE, Deehan M, Easson AM, Ecker D, Edwards D, Epemolu O, Evans L, Fields R, Francis S, Harradine P, Jeremiah F, Kiyoi T, McArthur D, Morrison A, Passier P, Pick J, Schnabel PG, Schulz J, Steinbrede H, Walker G, Westwood P, Wishart G, Udo de Haes J. Ratcliffe P, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2541-6. doi: 10.1016/j.bmcl.2011.02.023. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21411321
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI. Park Y, et al. Among authors: epemolu o. ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17. ACS Infect Dis. 2017. PMID: 27704782 Free PMC article.
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).
Soares P, Gadd MS, Frost J, Galdeano C, Ellis L, Epemolu O, Rocha S, Read KD, Ciulli A. Soares P, et al. Among authors: epemolu o. J Med Chem. 2018 Jan 25;61(2):599-618. doi: 10.1021/acs.jmedchem.7b00675. Epub 2017 Sep 18. J Med Chem. 2018. PMID: 28853884 Free PMC article.
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
Cleghorn LAT, Ray PC, Odingo J, Kumar A, Wescott H, Korkegian A, Masquelin T, Lopez Moure A, Wilson C, Davis S, Huggett M, Turner P, Smith A, Epemolu O, Zuccotto F, Riley J, Scullion P, Shishikura Y, Ferguson L, Rullas J, Guijarro L, Read KD, Green SR, Hipskind P, Parish T, Wyatt PG. Cleghorn LAT, et al. Among authors: epemolu o. J Med Chem. 2018 Aug 9;61(15):6592-6608. doi: 10.1021/acs.jmedchem.8b00172. Epub 2018 Jul 26. J Med Chem. 2018. PMID: 29944372 Free PMC article.
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.
Wilson C, Ray P, Zuccotto F, Hernandez J, Aggarwal A, Mackenzie C, Caldwell N, Taylor M, Huggett M, Mathieson M, Murugesan D, Smith A, Davis S, Cocco M, Parai MK, Acharya A, Tamaki F, Scullion P, Epemolu O, Riley J, Stojanovski L, Lopez-Román EM, Torres-Gómez PA, Toledo AM, Guijarro-Lopez L, Camino I, Engelhart CA, Schnappinger D, Massoudi LM, Lenaerts A, Robertson GT, Walpole C, Matthews D, Floyd D, Sacchettini JC, Read KD, Encinas L, Bates RH, Green SR, Wyatt PG. Wilson C, et al. Among authors: epemolu o. J Med Chem. 2022 Jan 13;65(1):409-423. doi: 10.1021/acs.jmedchem.1c01586. Epub 2021 Dec 15. J Med Chem. 2022. PMID: 34910486 Free PMC article.
39 results