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Fused Tetrahydroquinolines Are Interfering with Your Assay.
Bashore FM, Annor-Gyamfi J, Du Y, Katis V, Nwogbo F, Flax RG, Frye SV, Pearce KH, Fu H, Willson TM, Drewry DH, Axtman AD. Bashore FM, et al. Among authors: willson tm. J Med Chem. 2023 Nov 9;66(21):14434-14446. doi: 10.1021/acs.jmedchem.3c01277. Epub 2023 Oct 24. J Med Chem. 2023. PMID: 37874947 Free PMC article. Review.
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ. Trump RP, et al. Among authors: willson tm. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. doi: 10.1016/j.bmcl.2007.04.111. Epub 2007 May 18. Bioorg Med Chem Lett. 2007. PMID: 17533125
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
Chao EY, Caravella JA, Watson MA, Campobasso N, Ghisletti S, Billin AN, Galardi C, Wang P, Laffitte BA, Iannone MA, Goodwin BJ, Nichols JA, Parks DJ, Stewart E, Wiethe RW, Williams SP, Smallwood A, Pearce KH, Glass CK, Willson TM, Zuercher WJ, Collins JL. Chao EY, et al. Among authors: willson tm. J Med Chem. 2008 Sep 25;51(18):5758-65. doi: 10.1021/jm800612u. J Med Chem. 2008. PMID: 18800767
A public-private partnership to unlock the untargeted kinome.
Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ. Knapp S, et al. Among authors: willson tm. Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. Nat Chem Biol. 2013. PMID: 23238671 No abstract available.
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH. Chen P, et al. Among authors: willson tm. J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6. J Med Chem. 2016. PMID: 25799074 Free PMC article.
The promise and peril of chemical probes.
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ. Arrowsmith CH, et al. Among authors: willson tm. Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. Nat Chem Biol. 2015. PMID: 26196764 Free PMC article.
Comprehensive characterization of the Published Kinase Inhibitor Set.
Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ. Elkins JM, et al. Among authors: willson tm. Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26. Nat Biotechnol. 2016. PMID: 26501955
232 results