RLM Stability Data

Hepatic metabolic stability is a key pharmacokinetic parameter in drug discovery. Metabolic stability is usually assessed in microsomal fractions and only the best compounds progress in the drug discovery process. A high-throughput single time point substrate depletion method in rat liver microsomes (RLM) is employed at the National Center for Advancing Translational Sciences (NCATS) as a Tier 1 assay. This dataset has two files. First file (dataset_rlm_ncats.tab) contains 2528 compounds and the second file (drugs_rlm_ncats.tab) contains 220 approved drugs, both compound sets tested in the same RLM assay.

肝脏代谢稳定性是药物发现过程中的关键药代动力学参数。代谢稳定性通常通过微粒体组分进行评估，仅表现最佳的化合物能够进入药物发现流程的下一阶段。美国国家转化促进中心（National Center for Advancing Translational Sciences, NCATS）采用大鼠肝微粒体（rat liver microsomes, RLM）高通量单时间点底物消耗法作为一级检测（Tier 1 assay）方法。本数据集包含两个文件：第一个文件（dataset_rlm_ncats.tab）涵盖2528种化合物，第二个文件（drugs_rlm_ncats.tab）包含220种已获批药物，两类化合物均通过同一套大鼠肝微粒体检测体系完成测试。