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
|
|
-
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
|
|
- 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)。 |
|
|