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Resource Category: Publications

Discovery of potent DOT1L inhibitors by AlphaLISA based High Throughput Screening assay

Yakai Song et al. Bioorg Med Chem. 2018 May 1;26(8):1751-1758. doi: 10.1016/j.bmc.2018.02.020. Epub 2018 Feb 24.

Gambogenic acid inhibits fibroblast growth factor receptor signaling pathway in erlotinib-resistant non-small-cell lung cancer and suppresses patient-derived xenograft growth

Xu L, et al. Cell Death Dis. 2018 Feb 15;9(3):262. doi: 10.1038/s41419-018-0314-6.

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

Popovici-Muller J, et al. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. doi: 10.1021/acsmedchemlett.7b00421. eCollection 2018 Apr 12.

Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation

Chen Wang et al. J Med Chem. 2017 Nov 9;60(21):8888-8905. doi: 10.1021/acs.jmedchem.7b00587. Epub 2017 Oct 27.

A microfluidics-based mobility shift assay to identify new inhibitors of β-secretase for Alzheimer’s disease

Liu R, et al. A microfluidics-based mobility shift assay to identify new inhibitors of β-secretase for Alzheimer's disease. Anal Bioanal Chem. 2017 Nov;409(28):6635-6642. doi: 10.1007/s00216-017-0617-y. Epub 2017 Sep 9.

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model

Jun Liang et al. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4370-4376. doi: 10.1016/j.bmcl.2017.08.022. Epub 2017 Aug 12.

Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization

Mao R, Zhu K, Tao H, Song JL, Jin L, Zhang Y, Liu J, Chen Z, Jiang CS, Luo C, Zhang H. Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit

Machine-Learning-Assisted Approach for Discovering Novel Inhibitors Targeting Bromodomain-Containing Protein 4

Jing Xing et al. J Chem Inf Model. 2017 Jul 24;57(7):1677-1690.

Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate

Yong-Kang Zhang et al. J Med Chem. 2017 Jul 13;60(13):5889-5908. doi: 10.1021/acs.jmedchem.7b00621. Epub 2017 Jun 29.

Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders

Rudolph J, Svensson KA, Hao J, Li X, Matrisciano F, Meltzer HY. Neuropharmacology. 2018 Jan;128:351-365. doi: 10.1016/j.neuropharm.2017.10.032. Epub 2017 Oct 26.
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