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Page 1
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
Deaton DN, Do Y, Holt J, Jeune MR, Kramer HF, Larkin AL, Orband-Miller LA, Peckham GE, Poole C, Price DJ, Schaller LT, Shen Y, Shewchuk LM, Stewart EL, Stuart JD, Thomson SA, Ward P, Wilson JW, Xu T, Guss JH, Musetti C, Rendina AR, Affleck K, Anders D, Hancock AP, Hobbs H, Hodgson ST, Hutchinson J, Leveridge MV, Nicholls H, Smith IED, Somers DO, Sneddon HF, Uddin S, Cleasby A, Mortenson PN, Richardson C, Saxty G. Deaton DN, et al. Among authors: smith ied. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478. doi: 10.1016/j.bmc.2019.02.017. Epub 2019 Feb 11. Bioorg Med Chem. 2019. PMID: 30858025
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.
Borthwick AD, Liddle J, Davies DE, Exall AM, Hamlett C, Hickey DM, Mason AM, Smith IE, Nerozzi F, Peace S, Pollard D, Sollis SL, Allen MJ, Woollard PM, Pullen MA, Westfall TD, Stanislaus DJ. Borthwick AD, et al. J Med Chem. 2012 Jan 26;55(2):783-96. doi: 10.1021/jm201287w. Epub 2012 Jan 12. J Med Chem. 2012. PMID: 22239250
Optimization of a Series of RIPK2 PROTACs.
Miah AH, Smith IED, Rackham M, Mares A, Thawani AR, Nagilla R, Haile PA, Votta BJ, Gordon LJ, Watt G, Denyer J, Fisher DT, Dace P, Giffen P, Goncalves A, Churcher I, Scott-Stevens P, Harling JD. Miah AH, et al. Among authors: smith ied. J Med Chem. 2021 Sep 9;64(17):12978-13003. doi: 10.1021/acs.jmedchem.1c01118. Epub 2021 Aug 25. J Med Chem. 2021. PMID: 34432979
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N-Methylation for PI3Kδ Activity.
Barnes L, Blaber H, Brooks DTK, Byers L, Buckley D, Byron ZC, Chilvers RG, Cochrane L, Cooney E, Damian HA, Francis L, Fu He D, Grace JMJ, Green HJ, Hogarth EJP, Jusu L, Killalea CE, King O, Lambert J, Lee ZJ, Lima NS, Long CL, Mackinnon ML, Mahdy S, Matthews-Wright J, Millward MJ, Meehan MF, Merrett C, Morrison L, Parke HRI, Payne C, Payne L, Pike C, Seal A, Senior AJ, Smith KM, Stanelyte K, Stillibrand J, Szpara R, Taday FFH, Threadgould AM, Trainor RJ, Waters J, Williams O, Wong CKW, Wood K, Barton N, Gruszka A, Henley Z, Rowedder JE, Cookson R, Jones KL, Nadin A, Smith IE, Macdonald SJF, Nortcliffe A. Barnes L, et al. J Med Chem. 2019 Nov 27;62(22):10402-10422. doi: 10.1021/acs.jmedchem.9b01499. Epub 2019 Nov 6. J Med Chem. 2019. PMID: 31647659
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Alder CM, Ambler M, Campbell AJ, Champigny AC, Deakin AM, Harling JD, Harris CA, Longstaff T, Lynn S, Maxwell AC, Mooney CJ, Scullion C, Singh OM, Smith IE, Somers DO, Tame CJ, Wayne G, Wilson C, Woolven JM. Alder CM, et al. ACS Med Chem Lett. 2013 Aug 12;4(10):948-52. doi: 10.1021/ml400206q. eCollection 2013 Oct 10. ACS Med Chem Lett. 2013. PMID: 24900590 Free PMC article.
Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.
Hobbs CJ, Bit RA, Cansfield AD, Harris B, Hill CH, Hilyard KL, Kilford IR, Kitas E, Kroehn A, Lovell P, Pole D, Rugman P, Sherborne BS, Smith IE, Vesey DR, Walmsley DL, Whittaker D, Williams G, Wilson F, Banner D, Surgenor A, Borkakoti N. Hobbs CJ, et al. Bioorg Med Chem Lett. 2002 May 20;12(10):1365-9. doi: 10.1016/s0960-894x(02)00167-1. Bioorg Med Chem Lett. 2002. PMID: 11992778
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2.
Mares A, Miah AH, Smith IED, Rackham M, Thawani AR, Cryan J, Haile PA, Votta BJ, Beal AM, Capriotti C, Reilly MA, Fisher DT, Zinn N, Bantscheff M, MacDonald TT, Vossenkamper A, Dace P, Churcher I, Benowitz AB, Watt G, Denyer J, Scott-Stevens P, Harling JD. Mares A, et al. Among authors: smith ied. Commun Biol. 2020 Mar 20;3(1):140. doi: 10.1038/s42003-020-0868-6. Commun Biol. 2020. PMID: 32198438 Free PMC article.
A Phenotypic Approach for the Identification of New Molecules for Targeted Protein Degradation Applications.
Stacey P, Lithgow H, Lewell X, Konopacka A, Besley S, Green G, Whatling R, Law R, Röth S, Sapkota GP, Smith IED, Burley GA, Harling J, Benowitz AB, Queisser MA, Muelbaier M. Stacey P, et al. Among authors: smith ied. SLAS Discov. 2021 Aug;26(7):885-895. doi: 10.1177/24725552211017517. Epub 2021 May 27. SLAS Discov. 2021. PMID: 34041938 Free article.
12 results