MARV Inhibitor

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC₅₀=0.31, and 0.82 µM, respectively) and low cytotoxicity (SI>100) in HeLa cells.

EBOV/MARV-IN-2 (compound 13) is an Ebolavirus (EBOV, IC₅₀=0.9 μM) and Marburg virus (MARV, IC₅₀=2.7 μM) inhibitor.

As-358 has inhibitory effects against Ebola virus and Marburg virus, with IC₅₀s of 47.5 μM and 3.7 μM.

EBOV/MARV-IN-3 (compound 32) is a potent EBOV and MARV inhibitor with IC₅₀ values of 0.5, 1.2 µM, respectively. EBOV/MARV-IN-3 binds to the hydrophobic pocket close to EBOV Y517. EBOV/MARV-IN-3 shows antiviral activity.

As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC₅₀s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety.

CP19, a histamine receptor antagonist, is an entry inhibitor against both Ebolavirus (EBOV) and Marburgvirus (MARV) with IC₅₀s of 3.4 μM and 29.5 μM, respectively. CP19 has SI values of 29.4 and 3.4 for EBOV and MARV, respectively. CP19 has antiviral activity.