rdrp inhibitor

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

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.

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.

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.

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.

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.

SARS-CoV-2-IN-73 (compound 4) is an inhibitor of the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).

PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and has antiviral properties with broad-spectrum anti-influenza activity. PAN, as the N-terminal PA subunit of the polymerase-RNA complex, possesses a cap-dependent endonuclease (CEN) active site, facilitating RNA cleavage and initiating the synthesis of new RNA molecules. PAN endonuclease-IN-2 targets both influenza HA and RdRp complexes, thereby disrupting viral entry into host cells and impeding viral replication.

RH12 is a dual inhibitor of SARS-CoV-2-related RNA-dependent RNA polymerase (RdRp, IC50 of 4.42 nM) and human transmembrane serine protease 2 (TMPRSS2, IC50 of 4.2 nM). It demonstrates antiviral activity by inhibiting viral replication and absorption, showing 90.5% virucidal effect in Vero-E6 cells. Additionally, RH12 inhibits Calu-3 cell viability with an IC50 of 17.5 nM.

MePT-S-N-Pme is an inhibitor of SARS-CoV-2 RdRp activity. It significantly reduces reporter gene activity, with an IC50 of 7 μM in HEK 293 cells. MePT-S-N-Pme exhibits a mild inhibitory effect on nucleotide transferase activity and markedly inhibits SARS-CoV-2 replication in vitro.

Nsp12-IN-2 (Compound 8), a triphosphate metabolite of 4'-thiouridine, functions as an inhibitor of SARS-CoV-2 Nsp12. It effectively suppresses the RNA-dependent RNA polymerase (RdRp) activity of the SARS-CoV-2 Nsp12-Nsp7-Nsp8 complex, halting RNA synthesis and blocking the RNA capping and NMP capping of Nsp9. Nsp12-IN-2 shows potential for research into infections caused by SARS-CoV-2, other coronaviruses, and additional RNA viruses.

Anti-Influenza agent 10 (Compound 41) is an inhibitor of the RNA-dependent RNA polymerase (RdRp) of the influenza A virus. It shows potent antiviral activity against the A/PR/8/34(H1N1) strain, with an IC50 of 0.29 μM and a KD of 4.11 μM. The compound functions by disrupting the interaction between the PA and PB1 subunits, inhibiting the assembly of the viral RdRp complex, and thereby blocking transcription and replication of the viral genome. Anti-Influenza agent 10 also demonstrates significant broad-spectrum efficacy against various influenza strains, such as H3N2, H3N8, and H9N2, with IC50 values of 3.96, 1.91, and 1.45 μM, respectively. It is useful for research on influenza A virus infections.

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.

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.

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

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.