Some natural products generated from microorganisms show efficacies on the mechanisms of occurrence of human diseases, and thus provide precursors of drug development. Unfortunately, the discovery of such molecules relies on “the matter of luck” rather than a platform technology. We here conduct research to devise platform technologies that enable us to discover functional “natural product-like” molecules in a systematic manner. Such molecular technologies can lead a paradigm shift from a “by chance” to “reliable” drug discovery process, which brings about a new stream of innovation contributing to human health.