(Chemically synthesized)
Biological activity
tubulin inhibitor
Visual observation is a powerful approach for screening bioactive compounds that can facilitate the discovery of attractive druggable targets following their chemicobiological validation. So far, many high-content approaches, using sophisticated imaging technology and bioinformatics, have been developed. In our study, we aimed to develop a simpler method that focuses on intact cell images because we found that dynamic changes in morphology are informative, often reflecting the mechanism of action of a drug. Here, we constructed a chemical-genetic phenotype profiling system, based on the high-content cell morphology database Morphobase. This database compiles the phenotypes of cancer cell lines that are induced by hundreds of reference compounds, wherein those of well-characterized anticancer drugs are classified by mode of action. Furthermore, we demonstrate the applicability of this system in identifying NPD6689, NPD8617, and NPD8969 as tubulin inhibitors.
  • Futamura Y, Kawatani M, Kazami S, Tanaka K, Muroi M, Shimizu T, Tomita K, Watanabe N, Osada H.: Morphobase, an encyclopedic cell morphology database, and its use for drug target identification.
    Chem Biol, 19(12): 1620-1630 (2012) PMID: 23261605 [ doi: 10.1016/j.chembiol.2012.10.014 ]
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