S1482 |
Daclatasvir (BMS-790052)
|
Daclatasvir (BMS-790052, EBP883) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3. |
-
J Med Virol, 2024, 96(7):e29787
-
EMBO Mol Med, 2024, 16(4):870-884
-
J Virol, 2024, e0192123.
|
|
S1538 |
Telaprevir
|
Telaprevir is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM. |
-
J Virol, 2024, e0192123.
-
bioRxiv, 2023, 2023.11.22.568224
-
NPJ Digit Med, 2022, 5(1):83
|
|
S2794 |
Sofosbuvir
|
Sofosbuvir is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. |
-
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) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2. |
-
Cell Death Discov, 2022, 8(1:446)
-
J Virol, 2022, jvi0190621
-
Sci Rep, 2021, 11(1):19443
|
|
S1183 |
Danoprevir
|
Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. 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) is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1. |
-
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 is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) used for the treatment of chronic HCV genotype 1 and 3 infection. |
-
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) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection.
|
-
Sci Rep, 2021, 11(1):19443
-
Cancers (Basel), 2019, 11(10)E1407
-
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
|
|
S5015 |
Simeprevir
|
Simeprevir is a competitive, reversible, macrocyclic, noncovalent hepatitis C virus (HCV) NS3/4A protease inhibitor that acts directly against the hepatitis C virus. It has a medium inhibitory concentration (IC50) <13 nM for all HCV NS3/4A enzymes(genotypes 1a, 1b, 2, 4, 5, and 6), but has an IC50 value of 37 nM for genotype 3. |
-
Chemistry, 2022, e202202798.
-
Cell Rep, 2021, 35(7):109133
-
Viruses, 2021, 13(2)173
|
|
S4935 |
Asunaprevir
|
Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication. |
-
Int J Mol Sci, 2023, 10.3390/ijms242115535
-
Nature, 2022, 604(7904):146-151
-
Chemistry, 2022, e202202798.
|
|
S3728 |
Grazoprevir
|
Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively. |
-
Cell Res, 2024, 34(1):31-46
-
Cell Rep, 2021, 35(7):109133
-
Front Oncol, 2021, 11:803278
|
|
S3724 |
Velpatasvir
|
Velpatasvir (GS-5816,VEL) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. |
-
mBio, 2023, 10.1128/mbio.01318-23
-
Front Oncol, 2021, 11:803278
-
Front Microbiol, 2020, 10:2936
|
|
S5403 |
Ombitasvir (ABT-267)
|
Ombitasvir (ABT-267) is an inhibitor of the HCV non-structural protein 5A with antiviral activity. |
-
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) is a nonstructural (NS) protein 3/4A protease inhibitor. |
-
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) is a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase, targeting NS5B polymerase. |
-
J Virus Erad, 2022, 8(2):100074
|
|
S3395 |
Tegobuvir
|
Tegobuvir (TGV, GS 333126, GS-9190) is a non-nucleoside inhibitor of HCV RNA replication with proven antiviral activity in HCV-infected patients. |
|
|
S9641 |
Pibrentasvir (ABT-530)
|
Pibrentasvir (ABT-530) is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50 ranging from 1.4 pM to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6. |
|
|
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) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication. |
|
|
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. |
|
|
S2074 |
Mecarbinate
|
Mecarbinate (Dimecarbin) is a chemical intermediate of arbidol hydrochloride. |
|
|
E1243 |
Azvudine
|
Azvudine (RO-0622) is a novel nucleoside reverse transcriptase inhibitor with antiviral activity against human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV), potently inhibits HIV-1 (EC50 range 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). |
|
|
S1482 |
Daclatasvir (BMS-790052)
|
Daclatasvir (BMS-790052, EBP883) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3. |
- J Med Virol, 2024, 96(7):e29787
- EMBO Mol Med, 2024, 16(4):870-884
- J Virol, 2024, e0192123.
|
|
S1538 |
Telaprevir
|
Telaprevir is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM. |
- J Virol, 2024, e0192123.
- bioRxiv, 2023, 2023.11.22.568224
- NPJ Digit Med, 2022, 5(1):83
|
|
S2794 |
Sofosbuvir
|
Sofosbuvir is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. |
- 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) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2. |
- Cell Death Discov, 2022, 8(1:446)
- J Virol, 2022, jvi0190621
- Sci Rep, 2021, 11(1):19443
|
|
S1183 |
Danoprevir
|
Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. 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) is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1. |
- 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 is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) used for the treatment of chronic HCV genotype 1 and 3 infection. |
- 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) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection.
|
- Sci Rep, 2021, 11(1):19443
- Cancers (Basel), 2019, 11(10)E1407
- Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
|
|
S5015 |
Simeprevir
|
Simeprevir is a competitive, reversible, macrocyclic, noncovalent hepatitis C virus (HCV) NS3/4A protease inhibitor that acts directly against the hepatitis C virus. It has a medium inhibitory concentration (IC50) <13 nM for all HCV NS3/4A enzymes(genotypes 1a, 1b, 2, 4, 5, and 6), but has an IC50 value of 37 nM for genotype 3. |
- Chemistry, 2022, e202202798.
- Cell Rep, 2021, 35(7):109133
- Viruses, 2021, 13(2)173
|
|
S4935 |
Asunaprevir
|
Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication. |
- Int J Mol Sci, 2023, 10.3390/ijms242115535
- Nature, 2022, 604(7904):146-151
- Chemistry, 2022, e202202798.
|
|
S3728 |
Grazoprevir
|
Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively. |
- Cell Res, 2024, 34(1):31-46
- Cell Rep, 2021, 35(7):109133
- Front Oncol, 2021, 11:803278
|
|
S3724 |
Velpatasvir
|
Velpatasvir (GS-5816,VEL) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. |
- mBio, 2023, 10.1128/mbio.01318-23
- Front Oncol, 2021, 11:803278
- Front Microbiol, 2020, 10:2936
|
|
S5403 |
Ombitasvir (ABT-267)
|
Ombitasvir (ABT-267) is an inhibitor of the HCV non-structural protein 5A with antiviral activity. |
- 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) is a nonstructural (NS) protein 3/4A protease inhibitor. |
- 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) is a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase, targeting NS5B polymerase. |
- J Virus Erad, 2022, 8(2):100074
|
|
S3395 |
Tegobuvir
|
Tegobuvir (TGV, GS 333126, GS-9190) is a non-nucleoside inhibitor of HCV RNA replication with proven antiviral activity in HCV-infected patients. |
|
|
S9641 |
Pibrentasvir (ABT-530)
|
Pibrentasvir (ABT-530) is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50 ranging from 1.4 pM to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6. |
|
|
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) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication. |
|
|
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. |
|
|
S2074 |
Mecarbinate
|
Mecarbinate (Dimecarbin) is a chemical intermediate of arbidol hydrochloride. |
|
|
E1243 |
Azvudine
|
Azvudine (RO-0622) is a novel nucleoside reverse transcriptase inhibitor with antiviral activity against human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV), potently inhibits HIV-1 (EC50 range 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). |
|
|