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Page 1
Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.
Come JH, Senter TJ, Clark MP, Court JJ, Gale-Day Z, Gu W, Krueger E, Liang J, Morris M, Nanthakumar S, O'Dowd H, Maltais F, Iyer G, Andreassi J, Boucher C, Considine T, Moody CS, Taylor W, Mohanty AK, Huang Y, Zuccola H, Coll J, Bonanno KC, Gagnon KJ, Gan L, Lu F, Gao H, Chakilam A, Engtrakul J, Song B, Crawford D, Doyle E, Kramer T, Vought B, Phillips J, Kemper R, Sanders M, Swett R, Furey B, Winquist R, Bunnage ME, Jackson KL, Charifson PS, Magavi SS. Come JH, et al. Among authors: bunnage me. J Med Chem. 2021 Dec 23;64(24):17753-17776. doi: 10.1021/acs.jmedchem.1c00944. Epub 2021 Nov 8. J Med Chem. 2021. PMID: 34748351
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Boyd MJ, Collier PN, Clark MP, Deng H, Kesavan S, Ronkin SM, Waal N, Wang J, Cao J, Li P, Come J, Davies I, Duffy JP, Cochran JE, Court JJ, Chandupatla K, Jackson KL, Maltais F, O'Dowd H, Boucher C, Considine T, Taylor WP, Gao H, Chakilam A, Engtrakul J, Crawford D, Doyle E, Phillips J, Kemper R, Swett R, Empfield J, Bunnage ME, Charifson PS, Magavi SS. Boyd MJ, et al. Among authors: bunnage me. J Med Chem. 2021 Dec 23;64(24):17777-17794. doi: 10.1021/acs.jmedchem.1c00948. Epub 2021 Dec 6. J Med Chem. 2021. PMID: 34871500
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR. Gerstenberger BS, et al. Among authors: bunnage me. J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3. J Med Chem. 2016. PMID: 27115555 Free PMC article.
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD. Fish PV, et al. Among authors: bunnage me. J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8. J Med Chem. 2012. PMID: 23095041 Free PMC article.
Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.
Millan DS, Bunnage ME, Burrows JL, Butcher KJ, Dodd PG, Evans TJ, Fairman DA, Hughes SJ, Kilty IC, Lemaitre A, Lewthwaite RA, Mahnke A, Mathias JP, Philip J, Smith RT, Stefaniak MH, Yeadon M, Phillips C. Millan DS, et al. Among authors: bunnage me. J Med Chem. 2011 Nov 24;54(22):7797-814. doi: 10.1021/jm200677b. Epub 2011 Oct 28. J Med Chem. 2011. PMID: 21888439
The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics.
Rawson DJ, Ballard S, Barber C, Barker L, Beaumont K, Bunnage M, Cole S, Corless M, Denton S, Ellis D, Floc'h M, Foster L, Gosset J, Holmwood F, Lane C, Leahy D, Mathias J, Maw G, Million W, Poinsard C, Price J, Russel R, Street S, Watson L. Rawson DJ, et al. Bioorg Med Chem. 2012 Jan 1;20(1):498-509. doi: 10.1016/j.bmc.2011.10.022. Epub 2011 Oct 24. Bioorg Med Chem. 2012. PMID: 22100260
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.
Glossop PA, Watson CA, Price DA, Bunnage ME, Middleton DS, Wood A, James K, Roberts D, Strang RS, Yeadon M, Perros-Huguet C, Clarke NP, Trevethick MA, Machin I, Stuart EF, Evans SM, Harrison AC, Fairman DA, Agoram B, Burrows JL, Feeder N, Fulton CK, Dillon BR, Entwistle DA, Spence FJ. Glossop PA, et al. Among authors: bunnage me. J Med Chem. 2011 Oct 13;54(19):6888-904. doi: 10.1021/jm200884j. Epub 2011 Sep 20. J Med Chem. 2011. PMID: 21870878 Clinical Trial.
44 results