NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase ( NNRT ) with an IC 50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC 50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG ( IC 50 =25.9 µM) and CYP enzymes ( IC 50 >50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg).