先导化合物就是指通过生物测定，从众多的候选化合物中发现和选定的具有某种药物活性的新化合物，一般具有新颖的化学结构 其他的意思也有类似于引导出的意思
在药物研发过程中，先导化合物扮演着重要角色。它是指通过生物测定，从众多候选化合物中筛选出的具有某种药物活性的新化合物。这种化合物通常具有新颖的化学结构，能够为后续的药物设计和开发提供基础。先导化合物的发现和选择，是药物研发过程中的关键步骤。通过筛选，科研人员可以从大量的化合物中挑选出最有...
collated many of the published success stories of hit-to-lead optimization and analyzed them in ...
Hit-to-LeadShow advanced filters article Obstacles and innovations of macrocyclic drug development 16 January 2025 | By Ajay N Jain (VP of Research for the Optibrium’s BioPharmics Division), Ann E Cleves (VP of Application Science for Optibrium’s BioPharmics Division) Macrocycles outperform...
In the current study, the hit-to-lead optimization on the hit compound was explored in order to improve the SIRT binding and inhibition. Fourteen compounds, ten of which were new, have been synthesized and subjected to in vitro biological evaluation for their inhibitory activity against SIRT1-3...
Hit-to-lead stage of drug discovery is to refine each hit series to try to produce more potent and selective compounds which possess PK properties adequate to examine their efficacy in any in vivo models that are available. Typically, the work consists of intensive SAR investigations around each...
Hit to Lead (H2L), automated chemical synthesis and lead optimization workflows for faster screening cycles and to reduce the overall drug discovery timeline.
Hit to Lead also known as lead generation is a prerequisite for the construction of new drugs’ molecular structures and the key first step in the development of new drugs. This stage aims to obtain each hit series and try to produce more potent and selective compounds which possess pharmacokin...
As drug discovery enters the hit to lead stage, more detailed information on hit compounds is needed to guide the choice of the best compounds for the next step.Creative Biostructureprovides a variety of mainstream biophysical techniques for the identification and characterization of hit compounds. ...
Hit-to-lead optimization Latency-associated nuclear antigen (LANA) Kaposi’s sarcoma herpesvirus (KSHV) Fluorescence polarization (FP)-Based interaction inhibition assay Electrophoretic mobility shift assay (EMSA) CuAAC STD-NMR Abbreviations AIDS acquired immune deficiency syndrome CTD C-terminal domain DCM...