sars-cov-2-in-14

SARS-CoV-2-IN-14 is a potent and oral inhibitor of SARS-CoV-2 (IC50:0.39 μM), which is an analogue of niclosamide. SARS-CoV-2-IN-14 was more stable than niclosamide in the determination of human plasma and liver S9 enzyme. Oral administration of SARS-CoV-2-IN-14 can improve its bioavailability and half-life.

SARS-CoV-2 3CLpro-IN-14 (compound 11j) is an orally active inhibitor of SARS-CoV-2 3CLpro, demonstrating potent anti-SARS-CoV-2 properties with an EC50 of 0.18 μM and exhibits minimal cytotoxicity, having a CC50 greater than 50 μM, in Vero E6 cells [1].

Boceprevir (SCH 503034) is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.

NZ-804 is an orally active inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 of 8.9 nM. It inhibits replication of SARS-CoV-2 in HeLa-hACE2 cells, showing an EC50 of 14 nM. NZ-804 exhibits broad-spectrum antiviral activity against various CoVs and decreases viral replication in mice and hamster models.

RU-0415529 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (NSP14), with an IC50 of 356 nM. It inhibits viral RNA methylation and replication by stabilizing the cap-binding pocket through SAH binding. Additionally, RU-0415529 exhibits anti-infective activity in mouse models.

SARS-CoV-2 Mpro-IN-35 (compound 14) is an inhibitor of SARS-CoV-2 Mpro and is applicable in the study of the SARS-CoV-2 virus.

TDI-015051 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (SARS-CoV-2 NSP14) with an IC50 of ≤0.15 nM. It effectively inhibits SARS-CoV-2 NSP14 in Huh-7.5 cells (EC50=11.4 nM) and A549 cells expressing ACE2-TMPRSS2 (EC50=64.7 nM). Additionally, TDI-015051 suppresses other coronaviruses such as α-hCoV-NL63, α-hCoV-229E, and β-hCoV-MERS with IC50 values of 1.7, 2.6, and 3.6 nM, respectively. This compound inhibits viral RNA methylation and replication by binding to a stable SAH-cap pocket and demonstrates anti-infection activity in mouse models.

MMT5-14 is a SARS-CoV-2 inhibitor. MMT5-14 showed 2- to 7-fold higher antiviral activity in four variants of SARS-CoV-2. By reducing premature hydrolysis in hamsters, MMT5-14 increased the prodrug concentration by 200- to 300-fold in the plasma and lungs but also enhanced lung accumulation of the active metabolite triphosphate nucleosides (NTP) by 5-fold.

SARS-CoV-2 nsp14-IN-3 (4975) is a potent inhibitor of the N7-Methyltransferase activity of SARS-CoV-2 nonstructural protein 14 (Nsp14), with an IC50 value of 3.5 μM [1].