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Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Huang Y, Sendzik M, Zhang J, Gao Z, Sun Y, Wang L, Gu J, Zhao K, Yu Z, Zhang L, Zhang Q, Blanz J, Chen Z, Dubost V, Fang D, Feng L, Fu X, Kiffe M, Li L, Luo F, Luo X, Mi Y, Mistry P, Pearson D, Piaia A, Scheufler C, Terranova R, Weiss A, Zeng J, Zhang H, Zhang J, Zhao M, Dillon MP, Jeay S, Qi W, Moggs J, Pissot-Soldermann C, Li E, Atadja P, Lingel A, Oyang C. Huang Y, et al. Among authors: scheufler c. J Med Chem. 2022 Apr 14;65(7):5317-5333. doi: 10.1021/acs.jmedchem.1c02148. Epub 2022 Mar 30. J Med Chem. 2022. PMID: 35352560
Detecting S-adenosyl-L-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay.
Lin Y, Fan H, Frederiksen M, Zhao K, Jiang L, Wang Z, Zhou S, Guo W, Gao J, Li S, Harrington E, Meier P, Scheufler C, Xu YC, Atadja P, Lu C, Li E, Gu XJ. Lin Y, et al. Among authors: scheufler c. Anal Biochem. 2012 Apr 1;423(1):171-7. doi: 10.1016/j.ab.2012.01.019. Epub 2012 Jan 27. Anal Biochem. 2012. PMID: 22342622
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. Chen C, et al. Among authors: scheufler c. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563395 Free PMC article.
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C. Möbitz H, et al. Among authors: scheufler c. ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337327 Free PMC article.
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM. Smith A, et al. Among authors: scheufler c. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2017. PMID: 29107542
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse.
Stauffer F, Weiss A, Scheufler C, Möbitz H, Ragot C, Beyer KS, Calkins K, Guthy D, Kiffe M, Van Eerdenbrugh B, Tiedt R, Gaul C. Stauffer F, et al. Among authors: scheufler c. ACS Med Chem Lett. 2019 Dec 4;10(12):1655-1660. doi: 10.1021/acsmedchemlett.9b00452. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857842 Free PMC article.
Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R, Huppertz C. Schlapbach A, et al. Among authors: scheufler c. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6142-6. doi: 10.1016/j.bmcl.2008.10.039. Epub 2008 Oct 11. Bioorg Med Chem Lett. 2008. PMID: 18945615
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A. Velcicky J, et al. Among authors: scheufler c. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. doi: 10.1016/j.bmcl.2009.10.138. Epub 2009 Nov 3. Bioorg Med Chem Lett. 2010. PMID: 20060294
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Revesz L, Schlapbach A, Aichholz R, Dawson J, Feifel R, Hawtin S, Littlewood-Evans A, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C. Revesz L, et al. Among authors: scheufler c. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4719-23. doi: 10.1016/j.bmcl.2010.04.023. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20591669
36 results