hcov 229e in 1

HCoV-229E-IN-1 is a potent inhibitor of HCoV-229E replication, demonstrating efficacy with EC50 values of 0.65 μM in MTS cells and 0.6 μM in CPE cells[1].

HRSV hCoV-229E-IN-1 (compound 8X) is an effective inhibitor of HRSV and hCoV-229E, with an IC50 value of 2.1 µM for hCoV-229E. Additionally, HRSV hCoV-229E-IN-1 can inhibit cell viability.

HNC-1664 is an orally active inhibitor of RNA-dependent RNA polymerase (RdRP). It exhibits broad-spectrum antiviral activity against coronaviruses, including SARS-CoV-2 wild type and its variants (XBB.1.18, HK.3.1, BF.7.14, BA.1, HCoV-229E, HCoV-OC43), as well as arenaviruses. HNC-1664 also demonstrates anti-infective efficacy in a mouse model infected with the SARS-CoV-2 Delta variant.

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].

ARS-CoV-2-IN-53 (Compd 5d) shows an inhibitory effect on SARS-CoV-2 replication with an EC50 value of 14.3 μM and exhibits significant antiviral activity against human coronavirus 229E (HCoV-229E) [1].

BPR3P0128, a non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor, is effective orally and can inhibit various SARS-CoV-2 variants. It exhibits EC 50 values of 0.62 µM for SARS-CoV-2 and 0.14 µM for HCoV-229E, demonstrating potent anti-pancoronavirus activity at submicromolar concentrations. Additionally, BPR3P0128 displays synergistic antiviral effects when used in combination with Remdesivir [1].

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.