mers cov in 1

MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus and is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS).

SARS-CoV-2/MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, with IC50 values of 0.10 and 0.06 µM, respectively.

SARS-CoV-2-IN-1 is a potent inhibitor of Mpro [SARS-CoV-2 Mpro, SARS-CoV Mpro, and MERS-CoV Mpro] with IC50 values of 0.67, 0.90, and 0.58 μM, respectively.

SARS-CoV-2 Mpro-IN-37 (compound 8r) is an inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 value of 0.0199 μM. It exhibits IC50 values of 0.00945 μM against SARS-CoV-1 Mpro and 0.111 μM against MERS-CoV Mpro. SARS-CoV-2 Mpro-IN-37 demonstrates potent antiviral activity in the nanomolar range without showing cytotoxicity.

TMP1 is an orally active dual inhibitor targeting M pro (IC50= 312.5 nM) and TMPRSS2 (IC50= 1.28 μM, KD= 10.10 μM). It shows broad-spectrum protective effects in vitro against various SARS-CoV-2 variants. In vivo, TMP1 provides cross-protection against highly pathogenic coronaviruses, including SARS-CoV-1, SARS-CoV-2, and MERS-CoV, and effectively blocks the transmission of SARS-CoV-2. Additionally, TMP1 can inhibit the infection of SARS-CoV-2 escape mutants resistant to Nivolumab. TMP1 is useful in coronavirus research.

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].

SARS-CoV-2 3CLpro-IN-10(5d) is a potent inhibitor of the SARS-CoV-2 3CL protease with an IC50 value of 190 nM and demonstrates broad-spectrum antiviral activity, exhibiting IC50 values of 790 nM for SARS-CoV-1 and 70 nM for MERS-CoV.

SARS-CoV-2 3CLpro-IN-11(11d) is a broad-spectrum antiviral compound that inhibits the SARS-CoV-2 3CL protease with an IC50 of 140 nM, and also exhibits inhibitory activity against SARS-CoV-1 and MERS-CoV with IC50 values of 240 nM and 70 nM, respectively.

Imatinib Impurity E is a specific impurity found in Imatinib, an orally available inhibitor of multiple tyrosine kinases, including BCR/ABL, v-Abl, PDGFR, and c-kit. Imatinib (STI571) operates by semi-competitively inhibiting enzyme activity; it binds adjacent to the ATP binding site, inducing a closed or self-inhibited conformation [1] [2] [3] [4]. Additionally, Imatinib acts as an inhibitor against SARS-CoV and MERS-CoV [5].

Remdesivir de(ethylbutyl 2-aminopropanoate) is a recognized impurity in Remdesivir, a nucleoside analog demonstrating potent antiviral efficacy. It exhibits EC50 values of 74 nM against SARS-CoV and MERS-CoV in human airway epithelial (HAE) cells, and 30 nM against murine hepatitis virus in delayed brain tumor cells. Notably effective in vitro against SARS-CoV-2 (COVID-19) infection, Remdesivir has garnered attention for its application in controlling the spread of the virus, as supported by references [1] [2].

SARS-CoV-IN-5 (compound 49) is a high-selectivity, non-peptide, non-covalent 3CLpro inhibitor. It exhibits IC50 values of 38 nM, 21.1 nM, and 86 nM against the 3CLpro of SARS-CoV-1, SARS-CoV-2, and bat coronavirus WIV1, respectively. SARS-CoV-IN-5 inhibits the replication of the SARS-CoV-2 Delta variant with an EC50 of 0.272 μM. The compound notably reduces viral copy numbers in the lungs of K18-hACE2 transgenic mouse model. Furthermore, SARS-CoV-IN-5 demonstrates broad-spectrum antiviral activity against SARS-CoV-1, WIV1, MERS, HCoV-OC43, HCoV-229E, and HKU9, targeting these coronaviruses effectively.