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Several enzymes playing important roles in complement activation by processing the complement proteins. Among them, the plasma concentration of complement factor D (denoted as factor D) was reported to be the lowest among all complement related proteins and considered a rate-limiting enzyme. Acting on the upstream of AP, factor D cleaves complement factor B bound with C3b into the C3bBb complex11 . The ubiquitous role of factor D in AP activation led to the implication that inhibition of factor D can be an attractive strategy in the complement targeted therapy. Factor D belongs to the serine protease family12. Previous factor D inhibitor developments have led to the discovery of non-specific catalytic site inhibitors including coumarin derived covalent inhibitors.