ZINC58368839 inhibits P2X7 receptors by binding to the ATP-binding pocket of the receptor and demonstrates strong specificity towards human P2X7R over human P2X4R and rat P2X3R¹. It inhibits BzATP-induced Ca²⁺ responses in HEK–hP2X7 cells with IC₅₀ value of 4.8 µM¹.

P2X receptors are cationic trimeric channel complexes that function as ATP-gated Ca²⁺-permeable channels. They are considered to be an attractive therapeutic target. This family includes seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors are ubiquitously expressed, and particularly in cells of haematopoietic origin^1,2.