S1482 |
Daclatasvir (BMS-790052)
|
Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂,EC50为9-50 pM,在细胞培养中,作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。 |
-
J Med Virol, 2024, 96(7):e29787
-
EMBO Mol Med, 2024, 16(4):870-884
-
J Virol, 2024, e0192123.
|
|
S1538 |
Telaprevir
|
Telaprevir是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂,IC50为0.354 μM。 |
-
J Virol, 2024, e0192123.
-
bioRxiv, 2023, 2023.11.22.568224
-
NPJ Digit Med, 2022, 5(1):83
|
|
S2794 |
Sofosbuvir
|
Sofosbuvir是一种 HCV的NS5B polymerase抑制剂,用于治疗慢性丙型肝炎病毒(HCV)的感染。
|
-
J Med Virol, 2024, 96(7):e29787
-
PLoS One, 2024, 19(5):e0303265
-
mBio, 2023, 10.1128/mbio.01318-23
|
|
S1480 |
Lomibuvir (VX-222)
|
Lomibuvir (VX-222, VCH-222)是一种新型的,有效的,选择性的HCV聚合酶抑制剂,IC50为0.94-1.2 μM,作用于突变型M423T效果低15.3倍,作用于突变型I482L效果低108倍。Phase 2。 |
-
Cell Death Discov, 2022, 8(1:446)
-
J Virol, 2022, jvi0190621
-
Sci Rep, 2021, 11(1):19443
|
|
S1183 |
Danoprevir
|
Danoprevir 是一种肽类抑制剂,作用于丙型肝炎病毒(HCV)的NS3/4A蛋白酶,IC50为0.2-3.5 nM,抑制HCV 1A/1B/4/5/6基因型比抑制2B/3A基因型效果高10倍左右。Phase 2。 |
-
Antimicrob Agents Chemother, 2024, 68(4):e0137323.
-
Viruses, 2023, 15(4)981
-
Cell Rep Methods, 2023, 3(10):100599
|
|
S3733 |
Boceprevir
|
Boceprevir (EBP 520, SCH 503034)是一种口服的、直接作用于hepatitis C virus (HCV) protease的抑制剂,对NS3蛋白酶的Ki值为14 nM。在治疗慢性肝炎C(genotype 1)中,常与其他抗病毒共同给药。 |
-
Eur J Med Chem, 2024, 268:116202
-
Int J Mol Sci, 2024, 25(11)5767
-
SLAS Discov, 2024, S2472-5552(24)00043-1
|
|
S5062 |
Daclatasvir Dihydrochloride
|
Daclatasvir是一种具有口服活性的抗病毒剂,抑制HCV的NS5A区域,用于治疗慢性遗传型1和3类的HCV感染。 |
-
Commun Biol, 2022, 5(1):154
-
J Antimicrob Chemother, 2021, 76(7):1874-1885
-
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
|
|
S7579 |
Ledipasvir (GS5885)
|
Ledipasvir (GS5885) 是一种HCV NS5A polymerase抑制剂,用于治疗丙型肝炎病毒感染。
|
-
Sci Rep, 2021, 11(1):19443
-
Cancers (Basel), 2019, 11(10)E1407
-
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
|
|
S5015 |
Simeprevir
|
Simeprevir一种竞争性的、可逆的、非共价结合的大环hepatitis C virus (HCV) NS3/4A protease抑制剂,直接抑制HCV病毒。它对HCV NS3/4A(genotypes 1a, 1b, 2, 4, 5, and 6)的平均IC50值小于13 nM,而对genotype 3的IC50值为37 nM。 |
-
Chemistry, 2022, e202202798.
-
Cell Rep, 2021, 35(7):109133
-
Viruses, 2021, 13(2)173
|
|
S4935 |
Asunaprevir
|
Asunaprevir是具有口服活性的HCV NS3抑制剂。HCV NS3是病毒复制蛋白加工所必需的蛋白酶。 |
-
Int J Mol Sci, 2023, 10.3390/ijms242115535
-
Nature, 2022, 604(7904):146-151
-
Chemistry, 2022, e202202798.
|
|
S3728 |
Grazoprevir
|
Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂,HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。 |
-
Cell Res, 2024, 34(1):31-46
-
Cell Rep, 2021, 35(7):109133
-
Front Oncol, 2021, 11:803278
|
|
S3724 |
Velpatasvir
|
Velpatasvir (GS-5816,VEL) 是二代NS5A抑制剂,抑制丙型肝炎病毒(HCV)的复制。 |
-
mBio, 2023, 10.1128/mbio.01318-23
-
Front Oncol, 2021, 11:803278
-
Front Microbiol, 2020, 10:2936
|
|
S5403 |
Ombitasvir (ABT-267)
|
Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。 |
-
Commun Biol, 2022, 5(1):154
-
Sci Rep, 2021, 11(1):19443
-
bioRxiv, 2021, 2021.07.21.453274
|
|
S5402 |
Dasabuvir (ABT-333)
|
Dasabuvir (ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. |
-
J Virus Erad, 2022, 8(2):100074
-
mSphere, 2021, 6(6):e0062321
-
Sci Rep, 2021, 11(1):19443
|
|
S5720 |
Glecaprevir
|
Glecaprevir(ABT-493) is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a. |
-
Cell Rep, 2021, 35(7):109133
-
Sci Rep, 2021, 11(1):19443
-
BioRxiv, 2020, 10.1101/2020.12.13.422511
|
|
S5404 |
Paritaprevir (ABT-450)
|
Paritaprevir (ABT-450)是NS3/4A抑制剂。 |
-
Cell Rep, 2021, 35(7):109133
-
BioRxiv, 2020, 10.1101/2020.12.13.422511
|
|
S3800 |
Lycorine hydrochloride
|
Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity. |
-
Aging Cell, 2021, e13307
|
|
S5307 |
PSI-6206 (GS-331007)
|
PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶。 |
-
J Virus Erad, 2022, 8(2):100074
|
|
S3395 |
Tegobuvir
|
Tegobuvir (TGV, GS 333126, GS-9190) 是一种 HCV RNA replication 的非核苷抑制剂,在被HCV感染的患者中已证明具有抗病毒的活性。 |
|
|
S9641 |
Pibrentasvir (ABT-530)
|
Pibrentasvir (ABT-530) 是一种新型的泛基因型丙型肝炎病毒 hepatitis C virus (HCV) NS5A 抑制剂,其针对包含基因型1至6的NS5A的HCV复制子的EC50值为1.4 pM至5.0 pM。 |
|
|
S5394 |
Tizoxanide
|
Tizoxanide (Desacetyl-nitazoxanide), a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C. |
-
Mol Ther, 2024, S1525-0016(24)00340-X
-
Int J Mol Sci, 2024, 25(8)4413
|
|
E0097 |
Mericitabine
|
Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。 |
|
|
S5652 |
Elbasvir
|
Elbasvir (MK8742) is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype. |
|
|
E3597 |
Herba taxilli Extract
|
Herba Taxilli Extract是从桑寄生Taxillus sutchuenensis中提取的,可用作HCV NS3丝氨酸蛋白酶的抑制剂。 |
|
|
S2074 |
Mecarbinate
|
Mecarbinate (Dimecarbin) 是Arbidol Hydrochloride的化学中间体。 |
|
|
E1243 |
Azvudine
|
Azvudine (RO-0622)是一种新型核苷类逆转录酶抑制剂,对人类免疫缺陷病毒(human immunodeficiency virus, HIV)、乙型肝炎病毒(hepatitis B virus, HBV)和丙型肝炎病毒(hepatitis C virus, HCV)具有抗病毒活性,可有效抑制HIV-1 (EC50为0.03~6.92 nM)和HIV-2 (EC50为0.018~0.025 nM)。 |
|
|
S1482 |
Daclatasvir (BMS-790052)
|
Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂,EC50为9-50 pM,在细胞培养中,作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。 |
- J Med Virol, 2024, 96(7):e29787
- EMBO Mol Med, 2024, 16(4):870-884
- J Virol, 2024, e0192123.
|
|
S1538 |
Telaprevir
|
Telaprevir是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂,IC50为0.354 μM。 |
- J Virol, 2024, e0192123.
- bioRxiv, 2023, 2023.11.22.568224
- NPJ Digit Med, 2022, 5(1):83
|
|
S2794 |
Sofosbuvir
|
Sofosbuvir是一种 HCV的NS5B polymerase抑制剂,用于治疗慢性丙型肝炎病毒(HCV)的感染。
|
- J Med Virol, 2024, 96(7):e29787
- PLoS One, 2024, 19(5):e0303265
- mBio, 2023, 10.1128/mbio.01318-23
|
|
S1480 |
Lomibuvir (VX-222)
|
Lomibuvir (VX-222, VCH-222)是一种新型的,有效的,选择性的HCV聚合酶抑制剂,IC50为0.94-1.2 μM,作用于突变型M423T效果低15.3倍,作用于突变型I482L效果低108倍。Phase 2。 |
- Cell Death Discov, 2022, 8(1:446)
- J Virol, 2022, jvi0190621
- Sci Rep, 2021, 11(1):19443
|
|
S1183 |
Danoprevir
|
Danoprevir 是一种肽类抑制剂,作用于丙型肝炎病毒(HCV)的NS3/4A蛋白酶,IC50为0.2-3.5 nM,抑制HCV 1A/1B/4/5/6基因型比抑制2B/3A基因型效果高10倍左右。Phase 2。 |
- Antimicrob Agents Chemother, 2024, 68(4):e0137323.
- Viruses, 2023, 15(4)981
- Cell Rep Methods, 2023, 3(10):100599
|
|
S3733 |
Boceprevir
|
Boceprevir (EBP 520, SCH 503034)是一种口服的、直接作用于hepatitis C virus (HCV) protease的抑制剂,对NS3蛋白酶的Ki值为14 nM。在治疗慢性肝炎C(genotype 1)中,常与其他抗病毒共同给药。 |
- Eur J Med Chem, 2024, 268:116202
- Int J Mol Sci, 2024, 25(11)5767
- SLAS Discov, 2024, S2472-5552(24)00043-1
|
|
S5062 |
Daclatasvir Dihydrochloride
|
Daclatasvir是一种具有口服活性的抗病毒剂,抑制HCV的NS5A区域,用于治疗慢性遗传型1和3类的HCV感染。 |
- Commun Biol, 2022, 5(1):154
- J Antimicrob Chemother, 2021, 76(7):1874-1885
- Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
|
|
S7579 |
Ledipasvir (GS5885)
|
Ledipasvir (GS5885) 是一种HCV NS5A polymerase抑制剂,用于治疗丙型肝炎病毒感染。
|
- Sci Rep, 2021, 11(1):19443
- Cancers (Basel), 2019, 11(10)E1407
- Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
|
|
S5015 |
Simeprevir
|
Simeprevir一种竞争性的、可逆的、非共价结合的大环hepatitis C virus (HCV) NS3/4A protease抑制剂,直接抑制HCV病毒。它对HCV NS3/4A(genotypes 1a, 1b, 2, 4, 5, and 6)的平均IC50值小于13 nM,而对genotype 3的IC50值为37 nM。 |
- Chemistry, 2022, e202202798.
- Cell Rep, 2021, 35(7):109133
- Viruses, 2021, 13(2)173
|
|
S4935 |
Asunaprevir
|
Asunaprevir是具有口服活性的HCV NS3抑制剂。HCV NS3是病毒复制蛋白加工所必需的蛋白酶。 |
- Int J Mol Sci, 2023, 10.3390/ijms242115535
- Nature, 2022, 604(7904):146-151
- Chemistry, 2022, e202202798.
|
|
S3728 |
Grazoprevir
|
Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂,HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。 |
- Cell Res, 2024, 34(1):31-46
- Cell Rep, 2021, 35(7):109133
- Front Oncol, 2021, 11:803278
|
|
S3724 |
Velpatasvir
|
Velpatasvir (GS-5816,VEL) 是二代NS5A抑制剂,抑制丙型肝炎病毒(HCV)的复制。 |
- mBio, 2023, 10.1128/mbio.01318-23
- Front Oncol, 2021, 11:803278
- Front Microbiol, 2020, 10:2936
|
|
S5403 |
Ombitasvir (ABT-267)
|
Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。 |
- Commun Biol, 2022, 5(1):154
- Sci Rep, 2021, 11(1):19443
- bioRxiv, 2021, 2021.07.21.453274
|
|
S5402 |
Dasabuvir (ABT-333)
|
Dasabuvir (ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. |
- J Virus Erad, 2022, 8(2):100074
- mSphere, 2021, 6(6):e0062321
- Sci Rep, 2021, 11(1):19443
|
|
S5720 |
Glecaprevir
|
Glecaprevir(ABT-493) is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a. |
- Cell Rep, 2021, 35(7):109133
- Sci Rep, 2021, 11(1):19443
- BioRxiv, 2020, 10.1101/2020.12.13.422511
|
|
S5404 |
Paritaprevir (ABT-450)
|
Paritaprevir (ABT-450)是NS3/4A抑制剂。 |
- Cell Rep, 2021, 35(7):109133
- BioRxiv, 2020, 10.1101/2020.12.13.422511
|
|
S3800 |
Lycorine hydrochloride
|
Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity. |
- Aging Cell, 2021, e13307
|
|
S5307 |
PSI-6206 (GS-331007)
|
PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶。 |
- J Virus Erad, 2022, 8(2):100074
|
|
S3395 |
Tegobuvir
|
Tegobuvir (TGV, GS 333126, GS-9190) 是一种 HCV RNA replication 的非核苷抑制剂,在被HCV感染的患者中已证明具有抗病毒的活性。 |
|
|
S9641 |
Pibrentasvir (ABT-530)
|
Pibrentasvir (ABT-530) 是一种新型的泛基因型丙型肝炎病毒 hepatitis C virus (HCV) NS5A 抑制剂,其针对包含基因型1至6的NS5A的HCV复制子的EC50值为1.4 pM至5.0 pM。 |
|
|
S5394 |
Tizoxanide
|
Tizoxanide (Desacetyl-nitazoxanide), a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C. |
- Mol Ther, 2024, S1525-0016(24)00340-X
- Int J Mol Sci, 2024, 25(8)4413
|
|
E0097 |
Mericitabine
|
Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。 |
|
|
S5652 |
Elbasvir
|
Elbasvir (MK8742) is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype. |
|
|
E3597 |
Herba taxilli Extract
|
Herba Taxilli Extract是从桑寄生Taxillus sutchuenensis中提取的,可用作HCV NS3丝氨酸蛋白酶的抑制剂。 |
|
|
S2074 |
Mecarbinate
|
Mecarbinate (Dimecarbin) 是Arbidol Hydrochloride的化学中间体。 |
|
|
E1243 |
Azvudine
|
Azvudine (RO-0622)是一种新型核苷类逆转录酶抑制剂,对人类免疫缺陷病毒(human immunodeficiency virus, HIV)、乙型肝炎病毒(hepatitis B virus, HBV)和丙型肝炎病毒(hepatitis C virus, HCV)具有抗病毒活性,可有效抑制HIV-1 (EC50为0.03~6.92 nM)和HIV-2 (EC50为0.018~0.025 nM)。 |
|
|