E0052New |
Merafloxacin
|
Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
|
|
|
E1111New |
VV116
|
VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM. |
|
|
E1112New |
GS-621763
|
GS-621763, an orally bioavailable prodrug of GS-441524, shows a dose-dependent antiviral effect on SARS-CoV-2 reporter virus expressing nanoluciferase (SARS-CoV-2 nLUC) replication with an EC50 of 2.8 μM, also inhibits reporter SARS-CoV-2 expressing firefly luciferase (SARS-CoV-2 Fluc) replication with EC50 of 0.125 μM. |
|
|
E1131New |
S-217622
|
S-217622 (Ensitrelvir fumarate) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor with IC50 of 13 nM. |
|
|
E1174New |
NK01-63
|
NK01-63 (Coronastat) is a potent inhibitor of the SARS-CoV-2 3CL protease, which is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle. |
|
|
S0833 |
EIDD-1931
|
EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. |
-
Antiviral Res, 2022, 199:105273
-
Toxicol Lett, 2022, 362:50-58
-
J Med Virol, 2022, 10.1002/jmv.27650
|
|
S1183 |
Danoprevir (ITMN-191)
|
Danoprevir (ITMN-191, RG7227) 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. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Cell Rep, 2021, 35(7):109133
-
Sci Rep, 2021, 11(1):19443
|
|
S1185 |
Ritonavir (ABT-538)
|
Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis. |
-
Arch Toxicol, 2022, 96(7):2113-2122
-
Commun Biol, 2022, 5(1):154
-
J Virol, 2022, JVI0173021
|
|
S1289 |
Carmofur
|
Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cancer Cell, 2021, S1535-6108(21)00659-0
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S1322 |
Dexamethasone (MK-125)
|
Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. |
-
Cell Stem Cell, 2022, 29(4):545-558.e13
-
Blood, 2022, blood.2022016241
-
Hepatology, 2022, 10.1002/hep.32436
|
|
S1351 |
Ivermectin (MK-933)
|
Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
-
J Virol, 2021, JVI0148121
-
BMC Cancer, 2021, 21(1):1307
-
Nat Cell Biol, 2020,
|
|
S1380 |
Lopinavir (ABT-378)
|
Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
-
Pharmaceutics, 2022, 14(2)376
-
Commun Biol, 2022, 5(1):154
-
J Cell Biochem, 2022, 10.1002/jcb.30213
|
|
S1386 |
Nafamostat mesilate (FUT-175)
|
Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis. |
-
Immunol Res, 2022, 1-11
-
Genes Cells, 2022, 10.1111/gtc.12945
-
bioRxiv, 2021, 2021.03.31.437960
|
|
S1401 |
Tenofovir
|
Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections. |
-
Cancer Discov, 2022, candisc.1117.2021
-
Antiviral Res, 2022, 203:105348
-
Antiviral Res, 2021, S0166-3542(21)00068-1
|
|
S1538 |
Telaprevir (VX-950)
|
Telaprevir (VX-950, LY-570310, MP-424) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Cell Rep, 2021, 35(7):109133
-
Front Pharmacol, 2021, 12:773198
|
|
S1620 |
Darunavir Ethanolate
|
Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
-
J Virol, 2022, JVI0173021
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Sci Rep, 2021, 11(1):19443
|
|
S1680 |
Disulfiram (NSC 190940)
|
Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD). |
-
Free Radic Biol Med, 2022, 181:14-28
-
mBio, 2022, 10.1128/mbio.02739-21
-
J Leukoc Biol, 2022, 10.1002/JLB.5MA1121-644R
|
|
S1691 |
Praziquantel
|
Praziquantel is an anthelmintic effective against flatworms. |
-
Parasitology, 2020, 1-11
-
PLoS Negl Trop Dis, 2015, 9(3):e0003593
|
|
S1706 |
Lamivudine (BCH-189)
|
Lamivudine (BCH-189, GR109714X) is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase. |
-
Cancer Discov, 2022, candisc.1117.2021
-
J Virol, 2022, JVI0173021
-
Front Cardiovasc Med, 2021, 8:634774
|
|
S1759 |
Pitavastatin (NK-104) calcium
|
Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis. |
-
Autophagy, 2022, 1-19
-
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
-
Cancer Discov, 2021, candisc.0551.2021
|
|
S1835 |
Azithromycin (CP-62993)
|
Azithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S2071 |
Prulifloxacin (NM441)
|
Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
|
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
J Virol, 2021, JVI0177821
|
|
S2079 |
Moexipril HCl
|
Moexipril HCl (RS-10085) is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
|
|
S2169 |
Rosuvastatin (ZD4522) calcium
|
Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay. |
-
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
-
Cancers (Basel), 2021, 13(21)5543
-
Cell Death Dis, 2021, 12(1):78
|
|
S2485 |
Mitoxantrone (NSC-301739) 2HCl
|
Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cancers (Basel), 2021, 13(8)1954
|
|
S2823 |
Tideglusib (NP031112)
|
Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2. |
-
Int J Mol Med, 2022, 49(6)84
-
Nat Immunol, 2021, 10.1038/s41590-021-01090-1
-
J Virol, 2021, JVI.02393-20
|
|
S2851 |
Baricitinib (INCB028050)
|
Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
-
Blood, 2022, blood.2021012366
-
J Immunother Cancer, 2022, 10(1)e003766
-
Arthritis Rheumatol, 2022, 10.1002/art.42070
|
|
S2853 |
Carfilzomib (PR-171)
|
Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis. |
-
Mol Cell, 2022, 82(3):585-597.e11
-
Nat Commun, 2022, 13(1):2736
-
Cell Death Differ, 2022, 10.1038/s41418-022-00942-z
|
|
S2874 |
Camostat Mesilate
|
Camostat (FOY-305, FOY-S980) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Nat Commun, 2021, 12(1):866
-
Biomedicines, 2021, 9(4)437
|
|
S2926 |
TDZD-8
|
TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC. |
-
Sci Transl Med, 2020, 12(554):eaba3613
-
FASEB J, 2018, 32(7):3924-3935
-
Nat Commun, 2017, 1;8(1):1232
|
|
S3035 |
Daunorubicin (RP 13057) HCl
|
Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
-
Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7
-
Cell Rep, 2022, 39(1):110643
-
J Cell Biochem, 2022, 10.1002/jcb.30213
|
|
S3037 |
Bepotastine Besilate
|
Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
S3079 |
Atovaquone
|
Atovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Sci Rep, 2019, 9(1):536
-
Sci Transl Med, 2015, 7(290):290ra89
|
|
S3124 |
Dexamethasone Acetate
|
Dexamethasone (NSC 39471) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
-
Pharmaceutics, 2022, 14(2)400
-
Hematology, 2022, 27(1):32-42
-
Cell Rep, 2021, 36(2):109360
|
|
S3511 |
FOY251
|
FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection. |
|
|
S3724 |
Velpatasvir
|
Velpatasvir (GS-5816) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. |
-
Front Oncol, 2021, 11:803278
-
Drug Metab Dispos, 2020, 48(12):1264-1270
-
Front Microbiol, 2020, 10:2936
|
|
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. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Cell Rep, 2021, 35(7):109133
-
Front Pharmacol, 2021, 12:773198
|
|
S4028 |
Dexamethasone Sodium Phosphate
|
Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
-
Pharmaceutics, 2022, 14(2)400
-
Dis Model Mech, 2022, dmm.049109
-
Hematology, 2022, 27(1):32-42
|
|
S4157 |
Chloroquine diphosphate
|
Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
-
Bioact Mater, 2022, 18:459-470
-
Phytomedicine, 2022, 98:153958
-
Bone, 2022, 154:116262
|
|
S4282 |
Nelfinavir (AG 1343) Mesylate
|
Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
|
-
mBio, 2022, 13(1):e0304421
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Cell Rep, 2021, 35(10):109218
|
|
S4430 |
Hydroxychloroquine Sulfate (NSC 4375)
|
Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
|
-
Cell Rep, 2022, 39(3):110712
-
Cell Death Dis, 2022, 13(3):197
-
Neurosci Bull, 2022, 10.1007/s12264-022-00818-9
|
|
S4646 |
Ciclesonide
|
Ciclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases. |
-
mBio, 2022, 13(1):e0304421
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Drug Test Anal, 2020, 10.1002/dta.2917
|
|
S5250 |
Darunavir
|
Darunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Sci Rep, 2021, 11(1):19443
-
ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
|
|
S5754 |
Baricitinib phosphate
|
Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
-
Arthritis Res Ther, 2022, 24(1):43
-
Immunol Res, 2022, 10.1007/s12026-022-09261-4
-
J Immunother Cancer, 2021, 9(6)e002305
|
|
S5911 |
Bictegravir
|
Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
J Antimicrob Chemother, 2021, dkab276
|
|
S5940 |
Bepotastine
|
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
|
|
S6676 |
Ebselen
|
Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay. |
-
Viruses, 2021, 13(2)173
-
Antiviral Res, 2020, 182:104924
|
|
S6999 |
Chloroquine (NSC-187208)
|
Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity. |
-
Bioact Mater, 2022, 18:459-470
-
Redox Biol, 2022, 52:102292
-
Cell Death Dis, 2022, 13(2):150
|
|
S7262 |
Vidofludimus
|
Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
|
-
J Med Virol, 2022, 10.1002/jmv.27891
-
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
|
|
S7392 |
Loxistatin Acid (E-64C)
|
Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry. |
-
ACS Chem Biol, 2021, 16(9):1628-1643
-
Sci Signal, 2018, 11(518)eaao0422
-
Sci Signal, 2018, 11(518)eaao0422
|
|
S7393 |
Aloxistatin (E64d)
|
Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%. |
-
J Immunother Cancer, 2022, 10(3)e004129
-
Mol Plant Pathol, 2022, 10.1111/mpp.13192
-
EMBO J, 2021, e108050
|
|
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
|
|
S7947 |
PX-12
|
PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.
|
-
Br J Cancer, 2022, 10.1038/s41416-022-01835-1
-
Mol Biol Rep, 2022, 10.1007/s11033-022-07177-8
-
Free Radic Biol Med, 2020, S0891-5849(20)31609-9
|
|
S7975 |
Favipiravir (T-705)
|
Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
|
-
Nat Commun, 2022, 13(1):2256
-
Antiviral Res, 2022, 199:105273
-
Rapid Commun Mass Spectrom, 2022, e9255
|
|
S8279 |
Shikonin (C.I. 75535)
|
Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
-
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Mil Med Res, 2022, 9(1):22
|
|
S8932 |
Remdesivir (GS-5734)
|
Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. |
-
Nature, 2022, 10.1038/s41586-022-04474-x
-
Cell Rep, 2022, 39(4):110744
-
mBio, 2022, 13(2):e0370521
|
|
S8969 |
Molnupiravir (EIDD-2801)
|
Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
-
Antiviral Res, 2022, 203:105343
-
Antiviral Res, 2022, 199:105273
-
J Cell Biochem, 2022, 10.1002/jcb.30213
|
|
S9567 |
Indinavir Sulfate
|
Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS. |
-
J Cell Biochem, 2022, 10.1002/jcb.30213
-
Mol Metab, 2020, 29;101027
-
Antimicrob Agents Chemother, 2020, AAC.00872-20
|
|
S9731 |
PF-00835231
|
PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19. |
-
Mol Cell, 2022, S1097-2765(22)00433-6
-
Bioorg Med Chem Lett, 2022, 66:128732
-
Nat Commun, 2021, 12(1):6786
|
|
S9858New |
Lufotrelvir (PF-07304814)
|
PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.
|
|
|
S9866New |
Nirmatrelvir (PF-07321332)
|
Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.
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Antiviral Res, 2022, 203:105343
-
Clin Transl Sci, 2022, 10.1111/cts.13292
-
Res Sq, 2022, rs.3.rs-1662783
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S9963New |
paquinimod
|
Paquinimod (ABR 25757), a specific inhibitor of S100A8/A9, could rescue the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice. |
|
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E0052New |
Merafloxacin
|
Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
|
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E1111New |
VV116
|
VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM. |
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E1112New |
GS-621763
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GS-621763, an orally bioavailable prodrug of GS-441524, shows a dose-dependent antiviral effect on SARS-CoV-2 reporter virus expressing nanoluciferase (SARS-CoV-2 nLUC) replication with an EC50 of 2.8 μM, also inhibits reporter SARS-CoV-2 expressing firefly luciferase (SARS-CoV-2 Fluc) replication with EC50 of 0.125 μM. |
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E1131New |
S-217622
|
S-217622 (Ensitrelvir fumarate) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor with IC50 of 13 nM. |
|
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E1174New |
NK01-63
|
NK01-63 (Coronastat) is a potent inhibitor of the SARS-CoV-2 3CL protease, which is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle. |
|
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S0833 |
EIDD-1931
|
EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. |
- Antiviral Res, 2022, 199:105273
- Toxicol Lett, 2022, 362:50-58
- J Med Virol, 2022, 10.1002/jmv.27650
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S1183 |
Danoprevir (ITMN-191)
|
Danoprevir (ITMN-191, RG7227) 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. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Cell Rep, 2021, 35(7):109133
- Sci Rep, 2021, 11(1):19443
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S1185 |
Ritonavir (ABT-538)
|
Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis. |
- Arch Toxicol, 2022, 96(7):2113-2122
- Commun Biol, 2022, 5(1):154
- J Virol, 2022, JVI0173021
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S1289 |
Carmofur
|
Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cancer Cell, 2021, S1535-6108(21)00659-0
- Hum Cell, 2021, 34(6):1911-1918
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S1322 |
Dexamethasone (MK-125)
|
Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. |
- Cell Stem Cell, 2022, 29(4):545-558.e13
- Blood, 2022, blood.2022016241
- Hepatology, 2022, 10.1002/hep.32436
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S1351 |
Ivermectin (MK-933)
|
Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
- J Virol, 2021, JVI0148121
- BMC Cancer, 2021, 21(1):1307
- Nat Cell Biol, 2020,
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S1380 |
Lopinavir (ABT-378)
|
Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
- Pharmaceutics, 2022, 14(2)376
- Commun Biol, 2022, 5(1):154
- J Cell Biochem, 2022, 10.1002/jcb.30213
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S1386 |
Nafamostat mesilate (FUT-175)
|
Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis. |
- Immunol Res, 2022, 1-11
- Genes Cells, 2022, 10.1111/gtc.12945
- bioRxiv, 2021, 2021.03.31.437960
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S1401 |
Tenofovir
|
Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections. |
- Cancer Discov, 2022, candisc.1117.2021
- Antiviral Res, 2022, 203:105348
- Antiviral Res, 2021, S0166-3542(21)00068-1
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S1538 |
Telaprevir (VX-950)
|
Telaprevir (VX-950, LY-570310, MP-424) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Cell Rep, 2021, 35(7):109133
- Front Pharmacol, 2021, 12:773198
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S1620 |
Darunavir Ethanolate
|
Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
- J Virol, 2022, JVI0173021
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Sci Rep, 2021, 11(1):19443
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S1680 |
Disulfiram (NSC 190940)
|
Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD). |
- Free Radic Biol Med, 2022, 181:14-28
- mBio, 2022, 10.1128/mbio.02739-21
- J Leukoc Biol, 2022, 10.1002/JLB.5MA1121-644R
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S1691 |
Praziquantel
|
Praziquantel is an anthelmintic effective against flatworms. |
- Parasitology, 2020, 1-11
- PLoS Negl Trop Dis, 2015, 9(3):e0003593
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S1706 |
Lamivudine (BCH-189)
|
Lamivudine (BCH-189, GR109714X) is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase. |
- Cancer Discov, 2022, candisc.1117.2021
- J Virol, 2022, JVI0173021
- Front Cardiovasc Med, 2021, 8:634774
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S1759 |
Pitavastatin (NK-104) calcium
|
Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis. |
- Autophagy, 2022, 1-19
- Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
- Cancer Discov, 2021, candisc.0551.2021
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S1835 |
Azithromycin (CP-62993)
|
Azithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
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S2071 |
Prulifloxacin (NM441)
|
Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
|
- J Cell Biochem, 2022, 10.1002/jcb.30213
- J Virol, 2021, JVI0177821
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S2079 |
Moexipril HCl
|
Moexipril HCl (RS-10085) is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
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S2169 |
Rosuvastatin (ZD4522) calcium
|
Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay. |
- Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
- Cancers (Basel), 2021, 13(21)5543
- Cell Death Dis, 2021, 12(1):78
|
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S2485 |
Mitoxantrone (NSC-301739) 2HCl
|
Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cancers (Basel), 2021, 13(8)1954
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S2823 |
Tideglusib (NP031112)
|
Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2. |
- Int J Mol Med, 2022, 49(6)84
- Nat Immunol, 2021, 10.1038/s41590-021-01090-1
- J Virol, 2021, JVI.02393-20
|
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S2851 |
Baricitinib (INCB028050)
|
Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
- Blood, 2022, blood.2021012366
- J Immunother Cancer, 2022, 10(1)e003766
- Arthritis Rheumatol, 2022, 10.1002/art.42070
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S2853 |
Carfilzomib (PR-171)
|
Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis. |
- Mol Cell, 2022, 82(3):585-597.e11
- Nat Commun, 2022, 13(1):2736
- Cell Death Differ, 2022, 10.1038/s41418-022-00942-z
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S2874 |
Camostat Mesilate
|
Camostat (FOY-305, FOY-S980) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Nat Commun, 2021, 12(1):866
- Biomedicines, 2021, 9(4)437
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S2926 |
TDZD-8
|
TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC. |
- Sci Transl Med, 2020, 12(554):eaba3613
- FASEB J, 2018, 32(7):3924-3935
- Nat Commun, 2017, 1;8(1):1232
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S3035 |
Daunorubicin (RP 13057) HCl
|
Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
- Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7
- Cell Rep, 2022, 39(1):110643
- J Cell Biochem, 2022, 10.1002/jcb.30213
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S3037 |
Bepotastine Besilate
|
Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 10.1007/s13577-021-00579-z
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S3079 |
Atovaquone
|
Atovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Sci Rep, 2019, 9(1):536
- Sci Transl Med, 2015, 7(290):290ra89
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S3124 |
Dexamethasone Acetate
|
Dexamethasone (NSC 39471) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
- Pharmaceutics, 2022, 14(2)400
- Hematology, 2022, 27(1):32-42
- Cell Rep, 2021, 36(2):109360
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S3511 |
FOY251
|
FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection. |
|
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S3724 |
Velpatasvir
|
Velpatasvir (GS-5816) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. |
- Front Oncol, 2021, 11:803278
- Drug Metab Dispos, 2020, 48(12):1264-1270
- Front Microbiol, 2020, 10:2936
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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. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Cell Rep, 2021, 35(7):109133
- Front Pharmacol, 2021, 12:773198
|
|
S4028 |
Dexamethasone Sodium Phosphate
|
Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
- Pharmaceutics, 2022, 14(2)400
- Dis Model Mech, 2022, dmm.049109
- Hematology, 2022, 27(1):32-42
|
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S4157 |
Chloroquine diphosphate
|
Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
- Bioact Mater, 2022, 18:459-470
- Phytomedicine, 2022, 98:153958
- Bone, 2022, 154:116262
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S4282 |
Nelfinavir (AG 1343) Mesylate
|
Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
|
- mBio, 2022, 13(1):e0304421
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Cell Rep, 2021, 35(10):109218
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S4430 |
Hydroxychloroquine Sulfate (NSC 4375)
|
Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
|
- Cell Rep, 2022, 39(3):110712
- Cell Death Dis, 2022, 13(3):197
- Neurosci Bull, 2022, 10.1007/s12264-022-00818-9
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S4646 |
Ciclesonide
|
Ciclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases. |
- mBio, 2022, 13(1):e0304421
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Drug Test Anal, 2020, 10.1002/dta.2917
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S5250 |
Darunavir
|
Darunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Sci Rep, 2021, 11(1):19443
- ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
|
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S5754 |
Baricitinib phosphate
|
Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
- Arthritis Res Ther, 2022, 24(1):43
- Immunol Res, 2022, 10.1007/s12026-022-09261-4
- J Immunother Cancer, 2021, 9(6)e002305
|
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S5911 |
Bictegravir
|
Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- J Antimicrob Chemother, 2021, dkab276
|
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S5940 |
Bepotastine
|
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
|
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S6676 |
Ebselen
|
Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay. |
- Viruses, 2021, 13(2)173
- Antiviral Res, 2020, 182:104924
|
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S6999 |
Chloroquine (NSC-187208)
|
Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity. |
- Bioact Mater, 2022, 18:459-470
- Redox Biol, 2022, 52:102292
- Cell Death Dis, 2022, 13(2):150
|
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S7262 |
Vidofludimus
|
Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
|
- J Med Virol, 2022, 10.1002/jmv.27891
- Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
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S7392 |
Loxistatin Acid (E-64C)
|
Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry. |
- ACS Chem Biol, 2021, 16(9):1628-1643
- Sci Signal, 2018, 11(518)eaao0422
- Sci Signal, 2018, 11(518)eaao0422
|
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S7393 |
Aloxistatin (E64d)
|
Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%. |
- J Immunother Cancer, 2022, 10(3)e004129
- Mol Plant Pathol, 2022, 10.1111/mpp.13192
- EMBO J, 2021, e108050
|
|
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
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S7947 |
PX-12
|
PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.
|
- Br J Cancer, 2022, 10.1038/s41416-022-01835-1
- Mol Biol Rep, 2022, 10.1007/s11033-022-07177-8
- Free Radic Biol Med, 2020, S0891-5849(20)31609-9
|
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S7975 |
Favipiravir (T-705)
|
Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
|
- Nat Commun, 2022, 13(1):2256
- Antiviral Res, 2022, 199:105273
- Rapid Commun Mass Spectrom, 2022, e9255
|
|
S8279 |
Shikonin (C.I. 75535)
|
Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
- Adv Sci (Weinh), 2022, 10.1002/advs.202104055
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Mil Med Res, 2022, 9(1):22
|
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S8932 |
Remdesivir (GS-5734)
|
Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. |
- Nature, 2022, 10.1038/s41586-022-04474-x
- Cell Rep, 2022, 39(4):110744
- mBio, 2022, 13(2):e0370521
|
|
S8969 |
Molnupiravir (EIDD-2801)
|
Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
- Antiviral Res, 2022, 203:105343
- Antiviral Res, 2022, 199:105273
- J Cell Biochem, 2022, 10.1002/jcb.30213
|
|
S9567 |
Indinavir Sulfate
|
Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS. |
- J Cell Biochem, 2022, 10.1002/jcb.30213
- Mol Metab, 2020, 29;101027
- Antimicrob Agents Chemother, 2020, AAC.00872-20
|
|
S9731 |
PF-00835231
|
PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19. |
- Mol Cell, 2022, S1097-2765(22)00433-6
- Bioorg Med Chem Lett, 2022, 66:128732
- Nat Commun, 2021, 12(1):6786
|
|
S9858New |
Lufotrelvir (PF-07304814)
|
PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.
|
|
|
S9866New |
Nirmatrelvir (PF-07321332)
|
Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.
|
- Antiviral Res, 2022, 203:105343
- Clin Transl Sci, 2022, 10.1111/cts.13292
- Res Sq, 2022, rs.3.rs-1662783
|
|
S9963New |
paquinimod
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Paquinimod (ABR 25757), a specific inhibitor of S100A8/A9, could rescue the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice. |
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