Determination of the drug binding site within integrin CD11b/CD18

α/β integrin heterodimers are cell surface proteins involved in cellular communication. The integrin CD11b/CD18 is the predominant integrin found in neutrophils, macrophages and monocoytes and has been implicated as a signaling protein for the inflammation response. Recently, a class of small molecule drugs that activate the integrin CD11b/CD18 was reported. Using molecular docking experiments and site‐directed mutagenesis, we have identified a putative drug binding site in the ligand‐binding aA domain of CD11b, which suggest an allosteric activation of the integrin.