JTP-0157602 (JTP0157602) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 4.2 nM.JTP-0157602 exhibits potent antiviral activity against HIV-1 with EC90 of 138 nM.JTP-0157602 retained potent antiviral activity (EC50=1-6 nM) against a broad panel of recombinant viruses with INSTI-related resistant mutations, including multiple substitutions that emerged in clinical studies of INSTIs (IN strand transfer inhibitors (INSTIs).JTP-0157602 inhibited HIV-1 replication mainly during the late-phase of the replication cycle.JTP-0157602 binds to the LEDGF/p75 binding pocket of HIV-1 integrase (IN).
