rdrp

Galidesivir (BCX4430) is a broad-spectrum antiviral compound, an adenosine analog that inhibits viral RNA-dependent RNA polymerase (RdRp) activity.Galidesivir inhibits a wide range of RNA viral pathogens in vitro, and reduces lung infections in infected animals.

AS-136A is an orally active measles virus RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity that inhibits measles virus and blocks viral RNA synthesis.

Simeprevir (TMC435) is a potent HCV NS3/4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM.

GS-441524 was shown to be a safe and effective treatment for feline infectious peritonitis (FIP). The optimum dosage was found to be 4.0 mg/kg SC q24h for at least 12 weeks

Lomibuvir (VCH-222) is a selective, non-nucleoside allosteric inhibitor of HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC 50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo -initiated RNA synthesis [1].

HeE1-2Tyr, a pyridobenzothiazole compound, is a potent inhibitor of flavivirus RNA-dependent RNA polymerases (RdRp). It significantly inhibits the RdRp activity of West Nile, Dengue, and SARS-CoV-2 in vitro, with an IC50 of 27.6 µM.

RdRP-IN-9 (Compound 6b) is a reversible covalent allosteric inhibitor of RdRp, demonstrating substantial anti-coronavirus activity with an EC50 of 0.68 μM against HCoV-OC43. By reversibly acylating the Cys12 in the NiRAN domain of non-structural protein 12 (nsp 12), it exerts prolonged antiviral effects and shows synergistic anti-coronavirus activity with Molnupiravir.

SARS-CoV-2 RdRp-IN-1 (Compound PAP-2) is a potent inhibitor of SARS-CoV-2 RdRp with an EC50 value of 1.11 μM. This compound interacts directly with SARS-CoV-2 RdRp, effectively resisting exonuclease (ExoN) activity, and demonstrates broad-spectrum antiviral activity against coronaviruses.

Mpro/RdRp-IN-1 (Compound 1) is a dual-target inhibitor effective against SARS-CoV-2, targeting RdRp with an EC50 of 25.45 μM and Mpro with an IC50 of 125.4 μM. It exhibits an EC50 of 4.79 μM against HCoV-OC43 with a selectivity index (SI) of 10.89. Mpro/RdRp-IN-1 is used in SARS-CoV-2 infection research.

RdRP-IN-10 is an inhibitor of the RNA-dependent RNA polymerase (RdRp) in SARS-CoV-2, with an IC50 value of 5.78 μM. It forms a covalent bond with Cys114 of SARS-CoV-2 nsp8, disrupting the stable interaction between nsp8 and nsp12. RdRP-IN-10 effectively inhibits the RNA polymerization reaction mediated by SARS-CoV-2 RdRp without interfering with the RNA-RdRp complex binding and demonstrates antiviral activity in cell models. This compound is applicable for research related to SARS-CoV-2 infection.

RdRP-IN-4 (compound 11q) is an arylbenzohydrazide analogue, an orally active inhibitor of influenza A virus RNA-dependent RNA polymerase (RdRp) that directly binds the PB1 subunit of RdRp. RdRP-IN-4 inhibited H1N1 (A/PR/8/34) Flu A and Flu B strains (B/Lee/1940) in a dose-dependent manner with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 had a significant antiviral effect in infected mice.

Trans-RdRP-IN-5 is a potent inhibitor of the influenza virus RNA-dependent RNA polymerase (RdRP), with applications in influenza virus research.

Cis-RdRP-IN-5 is an effective inhibitor of the influenza virus RNA-dependent RNA polymerase (RdRP), employed in influenza virus research.

RdRP-IN-5 (compound 20), a potent inhibitor of the influenza virus RNA-dependent RNA polymerase (RdRP), has potential application in influenza research [1].

RdRP-IN-6 (compound 27) is an RNA-dependent RNA polymerase (RdRp) inhibitor with an IC90 value of 14.1 μM, and it shows potential applications in antiviral and anticancer research [1].

RdRP-IN-7, a RNA-dependent RNA polymerase (RdRp) inhibitor, demonstrates efficacy against SARS-CoV-2 infection with an inhibitory concentration (IC50) of 8.2 μM and (IC90) of 14.1 μM, alongside a cytotoxic concentration (CC90) of 79.1 μM, rendering it suitable for antiviral research [1].

RdRP-IN-2 is an RNA-dependent RNA polymerase (RdRp) inhibitor that significantly inhibits SARS-CoV-2 RdRp with an IC50 of 41.2 µM and also inhibits Feline coronavirus (FIPV) replication.

RdRP-IN-8 (compound 45) is an antiviral agent targeting influenza viruses. It inhibits the viral RNA-dependent RNA polymerase (RdRP) activity by disrupting the heterodimerization of the PA and PB1 subunits, with an IC50 value of 0.13 μM.

Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.

ERDRP-0519 is an orally bioavailable small-molecule inhibitor of the Measles virus (MeV) polymerase. It effectively prevents measles disease in squirrel monkeys (Saimiri sciureus) and exhibits potent inhibition of morbilliviruses in the nanomolar range.

GS-443902 trisodium (GS-441524 triphosphate trisodium), the active triphosphate metabolite of Remdesivir (GS-5734), serves as a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), displaying inhibitory concentrations (IC50) of 1.1 μM for RSV RdRp and 5 μM for HCV RdRp.

Favipiravir is a potent and selective RNA-dependent RNA polymerase inhibitor for the treatment of influenza virus infections.

PC786 is a potent and selective non-nucleoside RSV L-protein polymerase inhibitor for inhalation therapy of RSV infections, with antiviral activity against RSV-A (IC50=0.09-0.71 nM) and RSV-B (IC 50=1.3-50.6 nM), and the ability to inhibit RSV RNA-dependent RNA polymerase in HEp-2 cells ( RdRp).

Setrobuvir (ANA-598) is an orally active, highly selective non-nucleoside HCV NS5B polymerase inhibitor that inhibits new RNA synthesis and primer extension, with IC₅₀ values ranging from 4 to 5 nM. Setrobuvir exhibits high binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp. Setrobuvir is suitable for Antiviral drugs studies.