rdrp inhibitor

Setrobuvir (ANA-598) is an orally active non-nucleoside HCV NS5B polymerase inhibitor with inhibitory effects on de novo RNA synthesis and primer extension with IC50s between 4 and 5 nM. setrobuvir shows good binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp.

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.

LabMol-319 is a potent Zika virus (ZIKV) NS5 RdRp inhibitor with antiviral activity for the study of ZIKV virus.

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

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.

Galidesivir is a viral RNA-dependent RNA polymerase (RdRP) inhibitor and broad spectrum antiviral nucleotide.In vitro, galidesivir displays antiviral activity against a range of RNA viruses, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses, and flaviviruses (EC50values range from 3 μM to >100 μM). Galidesivir protects against Ebola and Marburg viral infection in animal models.

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

Sotetsuflavone, with an IC50 of 0.16 μM, stands as the most active compound in its series, acting as a potent inhibitor of DENV-NS5 RdRp (Dengue virus NS5 RNA-dependent RNA polymerase).

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).

SARS-CoV-IN-6 (Compound 17) acts as an inhibitor of SARS-CoV-1 and SARS-CoV-2 RdRp, demonstrating an IC50 value of 7.8 μM against SARS-CoV-2 RdRp. This compound reduces the cytopathic effects of single-round infectious particles (SRIP) infected with SARS-CoV-1 and SARS-CoV-2 replicons and inhibits the expression of SARS-CoVN proteins. The EC50 values for SRIP based on SARS-CoV-1 and SARS-CoV-2 replicons are 0.12 µM and 1.47 µM, respectively.

MTI013 is a selective inhibitor of SARS-CoV-2 nsp14 Mtase (IC50: 2.98 µM) and an antiviral agent (IC50: 10.33 µM in HCoV-229E infected Huh7 cells). Additionally, MTI013 demonstrates synergistic antiviral effects when used in conjunction with the RdRp inhibitor SHEN26.

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.

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.

13-TP is an inhibitor of SARS-CoV-2. It effectively suppresses in vitro RNA synthesis catalyzed by the central replication-transcription complex (C-RTC, nsp12-nsp7-nsp82) of SARS-CoV-2. 13-TP fully inhibits RdRp polymerase activity and obstructs the complete extension of some primer RNAs.

Azvudine hydrochloride (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI) with strong antiviral effects against HIV, HBV, and HCV. It demonstrates highly potent inhibition of HIV-1 (EC50 ranging from 0.03 to 6.92 nM) and HIV-2 (EC50 ranging from 0.018 to 0.025 nM), and effectively inhibits NRTI-resistant viral strains.

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

RSV IAV-IN-3 (compound 14'i) is a dual inhibitor of respiratory syncytial virus (RSV) with an EC50 of 2.92 μM and influenza A virus (IAV) with an EC50 of 1.90 μM. RSV IAV-IN-3 significantly inhibits luciferase activity in a dose-dependent manner (EC50: 3.89 μM) and suppresses IAV infection, RdRp activity, as well as post-entry replication of IAV and RSV.

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.

ZIKV-IN-1 is a potent inhibitor of Zika virus (EC50: 2.8 μM, EC90: 6.8 μM) with anti-ZIKV effects and low cytotoxicity, showing high affinity for the RdRp domain of ZIKV.

AVG-233 is an orally available RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity that blocks respiratory syncytial virus and SARS-CoV-2 replication.AVG-233 is used in the study of respiratory syncytial virus infections.

CYP2C19-IN-1 is a potent, non-genotoxic, non-hepatotoxic inhibitor of CYP2C19. CYP2C19-IN-1 inhibits RNA-dependent RNA polymerase (RdRP) (Ki: 6.16 μM) and can be used to study Zika virus (ZIKV) infection.

DENV-IN-4 is a potent inhibitor of DENV (DENV EC50=4.79 μM, Vero CC50>100 μM, SI>20.9), demonstrating antiviral efficacy through concentration-dependent reduction of DENV2 expression and inhibition of RNA-dependent RNA polymerase (RdRp) activity.

GSK5852 (GSK2485852) is an HCV NS5B RdRp polymerase inhibitor, inhibiting NS5B with an IC50 of 50 nM. It exhibits antiviral effects against the hepatitis C virus (HCV) with EC50 values of 3.0 nM for GT1a and 1.7 nM for GT1b.

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].