A drug screening method is disclosed. The drug screening method includes steps of screening a compound library to obtain a first group of compounds capable of binding to a wild type target screening the first group of compounds to obtain a second group of compounds capable of binding to a mutant site of a mutant target analyzing characteristics of binding sites of the wild type target and the mutant type target to obtain physico-chemical properties of the binding sites identifying a candidate from the second group of compounds according to the physico-chemical properties of the binding site and performing a bio-assay on inhibitory activity of the candidate.
