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3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.
Kerns JK, Busch-Petersen J, Fu W, Boehm JC, Nie H, Muratore M, Bullion A, Lin G, Li H, Davis R, Lin X, Lakdawala AS, Cousins R, Field R, Payne J, Miller DD, Bamborough P, Christopher JA, Baldwin I, Osborn RR, Yonchuk J, Webb E, Rumsey WL. Kerns JK, et al. Among authors: nie h. ACS Med Chem Lett. 2018 Oct 30;9(12):1164-1169. doi: 10.1021/acsmedchemlett.8b00291. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613320 Free PMC article.
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.
Miller DD, Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ. Miller DD, et al. Among authors: nie h. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2255-8. doi: 10.1016/j.bmcl.2011.02.107. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21429745
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
Norton D, Bonnette WG, Callahan JF, Carr MG, Griffiths-Jones CM, Heightman TD, Kerns JK, Nie H, Rich SJ, Richardson C, Rumsey W, Sanchez Y, Verdonk ML, Willems HMG, Wixted WE, Wolfe L 3rd, Woolford AJ, Wu Z, Davies TG. Norton D, et al. Among authors: nie h. J Med Chem. 2021 Nov 11;64(21):15949-15972. doi: 10.1021/acs.jmedchem.1c01351. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34705450
Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2H-Chromen-2-One, in Cellular and In Vivo Models of Pulmonary Oxidative Stress.
Yonchuk JG, Foley JP, Bolognese BJ, Logan G, Wixted WE, Kou JP, Chalupowicz DG, Feldser HG, Sanchez Y, Nie H, Callahan JF, Kerns JK, Podolin PL. Yonchuk JG, et al. Among authors: nie h. J Pharmacol Exp Ther. 2017 Oct;363(1):114-125. doi: 10.1124/jpet.117.241794. Epub 2017 Aug 8. J Pharmacol Exp Ther. 2017. PMID: 28790194
1,943 results