HIV-1 inhibitor-16

HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity[1].

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

HIV-1 (WT):1.3 nM (EC50)

HIV-1 (K103N):5.4 nM (EC50)

HIV-1 (E138K):9.2 nM (EC50)

HIV-1 (Y181C):22 nM (EC50)

HIV-1 (L100I):35 mM (EC50)

[1]. Ding L, et al. Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. J Med Chem. 2022;65(3):2122-2138.