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: Combinatorial library method significantly accelerates molecular discovery and identification in many areas of biology and medicine. Current applied array technique and split-mix approach both have their own limitations. With this view, one-disc-one compound (ODOC) concept was first proposed and aimed to be applied to split-mix peptide library synthesis with the purpose of combining large-scale combinatorial synthesis and digital molecular identification as a whole. The constructed ODOC library may not only overcome the limitation of relatively small library size for array techniques, but substantially reduce the cost and tedious procedure of peptide sequencing for OBOC method through decoding the barcode on the discs. Therefore, the success of ODOC carriers on microfluidic split-mix peptide synthesis may solve the bottlenecks of both array techniques and OBOC method, increase the efficiency of drug discovery and make a potential impact on modern pharmaceutical industries.

Digital One-Disc-One-Compound Method for High-Throughput Discovery of Prostate Cancer-Targeting Ligands