Advances in Lead Generation

被引:20
作者
Holenz, Joerg [1 ,3 ]
Stoy, Patrick [2 ]
机构
[1] GlaxoSmithKline Pharmaceut LLC, 196 Broadway, Cambridge, MA 02139 USA
[2] GlaxoSmithKline Pharmaceut LLC, 1250 South Collegeville Rd, Collegeville, PA 19426 USA
[3] Grunenthal USA Inc, Cambridge Innovat Ctr, 14th Floor,1 Broadway, Cambridge, MA 02142 USA
关键词
Lead Generation; Hit Identification; Lead discovery; Hit to Lead; Screening methods; DRUG DISCOVERY; LIGAND EFFICIENCY; INHIBITOR; IMPACT; HIT; CANDIDATES; BIOPHYSICS; CHALLENGES; STRATEGIES; CHEMISTRY;
D O I
10.1016/j.bmcl.2018.12.001
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Lead Generation represents a critical drug discovery phase where chemical starting points and their respective mechanism of action, quality, and potential liabilities are largely predefined. Recent advances such as DNA-encoded libraries or fragment-, chemical biology-, and virtual screening-based approaches are today as common as traditional High Throughput Screening. Innovations in characterizing lead quality have allowed more informed decision-making by discovery teams. The key challenge today is to individually tailor the right mix of methods for each project to facilitate data integration with the purpose of creating multiple high-quality lead series, ultimately translating to reduced chemistry-related pipeline attrition.
引用
收藏
页码:517 / 524
页数:8
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