Development of small molecule modulators of WDR5/MLL1 protein-protein binding (Chemical Biology Consortium/NCI Experimental Therapeutics Collaboration)

在此期间，项目团队通过对十几种类似物进行细胞热位移测定（CETSA）数据，支持了更大规模的WDR 5合作，并开发了一种强大的CETSA分析算法，以帮助数据解释。 作为一个中心，NCGC与NIH和校外研究人员建立并保持了130多个积极的合作关系，促进了整个人类疾病领域的药物发现工作。这些努力已经导致了数十个高通量筛选和一些药物化学活动，以进一步改善筛选命中，为我们的合作者和一般研究社区提供出版物和各种有前途的小分子探针和线索。此外，NCGC还致力于推进多项信息化举措，以更好地利用现有的药物和疾病靶点信息，并为公众提供易于获取的资源，进一步促进人类疾病新疗法的开发。

During this period, the project team has supported the larger WDR5 collaboration by conducting cellular thermal shift assay (CETSA) data for dozen of analogs, and developed a robust CETSA analysis algorithm to aid with data interpretation. As a center, the NCGC has fostered and maintained over 130 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.