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Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors.
Veerman JJN, Bruseker YB, Damen E, Heijne EH, van Bruggen W, Hekking KFW, Winkel R, Hupp CD, Keefe AD, Liu J, Thomson HA, Zhang Y, Cuozzo JW, McRiner AJ, Mulvihill MJ, van Rijnsbergen P, Zech B, Renzetti LM, Babiss L, Müller G. Veerman JJN, et al. Among authors: van rijnsbergen p. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562. doi: 10.1021/acsmedchemlett.0c00547. eCollection 2021 Apr 8. ACS Med Chem Lett. 2021. PMID: 33859795 Free PMC article.
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T. Cai J, et al. Among authors: van rijnsbergen p. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. doi: 10.1016/j.bmcl.2010.10.012. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2010. PMID: 21030256