non-nucleoside polymerase

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.

TMC647055 Choline Hydroxide Salt is a novel and potent non-nucleoside inhibitor of the HCV NS5B polymerase which potentially for the treatment of HCV infection. It has nanomolar cellular potency (EC(50) of 82 nM) with minimal associated cell toxicity (CC(

Dasabuvir (ABT-333) is a non-nucleoside inhibitor of the hepatitis C virus (HCV) non-structural protein 5B (NS5B), an RNA-dependent RNA polymerase. Upon administration and intracellular uptake, dasabuvir binds HCV NS5B polymerase, blocking viral RNA synthesis and replication. The HCV NS5B protein is essential for the replication of the HCV RNA genome.

JNJ-7184 is a non-nucleoside inhibitor of the RSV-Large (L) polymerase, with pEC50 and pCC50 values of 7.86 and 4.29, respectively, in Hela cells. It inhibits the initiation or early elongation phases, thereby preventing RSV replication and transcription.

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].

Cis-Lomibuvir (cis-VX-222), a cis-isomer of Lomibuvir, is a selective non-nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase (RdRp), targeting thumb pocket 2 with a dissociation constant (Kd) of 17 nM. It exhibits an EC50 of 5.2 nM against the 1b/Con1 HCV subgenomic replicon, demonstrating a preference for inhibiting elongative RNA synthesis over de novo-initiated RNA synthesis.

CI-39, a natural antiviral product, serves as a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting wild type HIV-1. It exhibits an effective concentration (EC50) of 3.40 µM against the virus, while its cytotoxic concentration (CC50) exceeds 30 µM. This compound notably impedes HIV-1 reverse transcriptase (RT) DNA polymerase and ribonuclease H activities[1].

Deleobuvir(BI207127) is an inhibitor of non-nucleoside hepatitis C virus NS5B polymerase for the treatment of hepatitis C.

JTK-853 is a novel, non-nucleoside inhibitor of Hepatitis C Virus (HCV) polymerase, exhibiting effective antiviral activity in HCV replicon cells with EC50s of 0.38 μM for genotype 1a H77 strain and 0.035 μM for genotype 1b Con1 strain.

6-Hydroxypyridin-3-ylboronic acid is a heterocyclic building block.1,2It has been used in the synthesis of non-nucleoside inhibitors of hepatitis C virus (HCV) RNA-dependent RNA polymerase nonstructural protein 5B (NS5B).16-Hydroxypyridin-3-ylboronic acid has also been used in the synthesis of mammalian target of rapamycin (mTOR) inhibitors.2 1.Hendricks, R.T., Spencer, S.R., Blake, J.F., et al.3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymeraseBioorg. Med. Chem. Lett.19(2)410-414(2009) 2.Verheijen, J.C., Richard, D.J., Curran, K., et al.Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and sselective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituentJ. Med. Chem.52(24)8010-8024(2009)

ABT-072, also known as potassium trihydrate, is a highly effective non-nucleoside inhibitor of the HCV NS5B polymerase, administered orally. This compound exhibits potent activity against HCV GT1a (with an EC50 of 1 nM) and HCV GT1b (with an EC50 of 0.3 nM).

Deleobuvir sodium is the salt form of Deleobuvir, also known as BI207127, a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C. Deleobuvir was tested in combination regimens with pegylated interferon and ribavirin, and in interferon-free regimens with other direct-acting antiviral agents including faldaprevir. Deleobuvir showed that a triple combination of deleobuvir, faldaprevir, and ribavirin performed well in HCV genotype 1b patients. Efficacy fell below 50%, however, for dual regimens without ribavirin and for genotype 1a patients. In December 2013, deleobuvir was discontinued since recent findings from phase III trials did not suggest sufficient efficacy.

GS-441524 is a potent inhibitor of feline infectious peritonitis (FIP) virus with an EC50 of 0.78 μM.. GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. GS-441524 is a molecular precursor to a pharmacologically active nucleoside triphosphate molecule. These analogs act as an alternative substrate and RNA-chain terminator of viral RNA dependent RNA polymerase. GS-441524 was non-toxic in feline cells at concentrations as high as 100 uM and effectively inhibited FIPV replication in cultured CRFK cells and in naturally infected feline peritoneal macrophages at concentrations as low as 1 uM. Note: GS-441524 is an active metabolite of Remdesivir.

Dasabuvir (ABT-333) sodium is a non-nucleoside hepatitis C virus (HCV) polymerase inhibitor that exhibits inhibition of the RNA-dependent RNA polymerase (RNA polymerase) encoded by the HCV NS5B gene. Dasabuvir sodium inhibited genotype 1a (strain H77) replicon (EC50: 7.7 nM) and 1b (strain Con1) replicon (EC50: 1.8 nM).

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].