Advanced development of human KDM5 inhibitors (Chemical Biology Consortium/NCI Experimental Therapeutics Collaboration)

人类 KDM5 抑制剂的先进开发（化学生物学联盟/NCI 实验治疗合作组织）

• 批准号: 9358285
• 负责人: Ajit Jadhav
• 金额: $ 3.75万
• 依托单位: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/9358285
• 关键词: Advanced Development; Biological Assay; Biology; Chemicals; Collaborations; Communities; Development; Disease; Extramural Activities; Fostering; General Population; Genomics; Goals; Human; Informatics; Investigational Therapies; Lead; Modeling; Pharmaceutical Chemistry; Pharmaceutical Preparations; Process; Publications; Research; Research Personnel; Resources; Synthesis Chemistry; United States National Institutes of Health; Validation; Work; assay development; base; drug development; drug discovery; high throughput screening; human disease; improved; inhibitor/antagonist; new technology; novel; novel therapeutics; screening; small molecule; small molecule libraries; small molecule therapeutics; therapeutic development; tool

During this period, the NCATS group, as part of the KDM5 collaborative team, has worked to develop a large panel of HTS-amenable assays in a number of orthogonal formats, perform primary screening against a number of small molecule libraries, and pursue medicinal chemistry to further refine compound potencies. As a center, the NCGC has fostered and maintained over 110 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to dozens of high-throughput screens and a number of medicinal chemistry campaigns to further improve on screening hits, providing our collaborators and the general research community with publications and a variety of promising small molecule probes and leads. In addition, the NCGC has worked to advance a number of informatic initiatives to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.

在此期间，作为KDM5合作团队的一部分，NCATS小组已经努力开发了一系列适合高温高温试验的正交试验，对一些小分子文库进行初步筛选，并进行药物化学研究，以进一步完善化合物的效力。