non-nucleoside polymerase

Setrobuvir (ANA-598) 是一种口服活性非核苷类HCV NS5B 聚合酶抑制剂，对新的RNA 合成和引物延伸具有抑制作用，IC50s 在4到5nM 之间。Setrobuvir 对SARS-CoV-2 RdRp 显示出很好的结合亲和力，能诱导RdRp 受到抑制。

TMC647055 Choline Hydroxide Salt 是一种新型有效的 HCV NS5B 聚合酶非核苷抑制剂，可用于治疗 HCV 感染。它具有纳摩尔级细胞效力（EC(50) 为 82 nM），相关细胞毒性较小（CC(50)>20 μM），在大鼠和狗中具有良好的药代动力学特征。 TMC647055 显示出有体外生化、动力学和病毒学特征的前景。

Dasabuvir (ABT-333) 是丙型肝炎病毒非结构蛋白 5B 的非核苷抑制剂，是一种 RNA 依赖性 RNA 聚合酶，具有抗 HCV 的潜在活性。

BPR3P0128是一种口服活性非核苷类RNA依赖性RNA聚合酶 (RdRp) 抑制剂，可抑制各种SARS-CoV-2变异体活性，对SARS-CoV-2和HCoV-229E的EC50分别为0.62和0.14 µM，在亚微摩尔范围内具有高效抗泛冠状病毒活性，并与Remdesivir联用表现出协同抗病毒活性。

JNJ-7184, 作为一种非核苷类RSV-Large (L)聚合酶抑制剂，在Hela细胞中展现了其pEC50和pCC50的值分别为7.86和4.29。该化合物能够通过抑制RSV的复制和转录过程中的起始或早期延长阶段，有效阻止病毒活动。

cis-Lomibuvir (cis-VX-222) 是 Lomibuvir 的顺式异构体。Lomibuvir (VX-222) 是一种选择性的非核苷聚合酶抑制剂，靶向丙型肝炎病毒 NS5B 聚合酶 (RdRp) 的拇指口袋 2，Kd 为 17 nM。Lomibuvir 抑制 1b/Con1 型 HCV 亚基因组复制子，EC50为 5.2 nM。Lomibuvir 优先抑制延长的 RNA 合成，而非从头合成的 RNA。

CI-39 是一种抗病毒天然产物。CI-39 是一种 NNRTI (非核苷类逆转录酶抑制) 抗病毒剂，对野生型HIV 的EC50为 3.40 µM，CC50>30 µM。CI-39 抑制HIV-1RT DNA 聚合酶和核糖核酸酶 H 活性。

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. It also displays effective antiviral activity in HCV replicon cells (EC50s: 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively).

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.

Lomibuvir (VCH-222) 是丙型肝炎病毒 NS5B 聚合酶的一种非核苷变构抑制剂，Kd 值为 17 nM，已证明具有临床疗效。Lomibuvir 抑制 1b Con1 型 HCV 亚基因组复制子，EC50为 5.2 nM。Lomibuvir 优先抑制延长的 RNA 合成，而非从头合成的 RNA。

Dasabuvir (ABT-333) sodium 是非核苷丙型肝炎病毒 (HCV) 聚合酶抑制剂。Dasabuvir sodium 对 HCV NS5B 基因编码的 RNA 依赖性 RNA 聚合酶 (RNA polymerase) 表现出抑制作用。Dasabuvir sodium 能够抑制基因型 1a (菌株 H77) 复制子 (EC50: 7.7 nM) 和 1b (菌株 Con1) 复制子 (EC50: 1.8 nM)。

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.