-
PDGFR inhibitor
Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.- Rong Zhang, .et al. , Gene, 2024, Jan 30:893:147917 PMID: 37866664
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Takafumi Shima, .et al. , Oncol Rep, 2022, 47: 7 PMID: 34738628
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- BM Duggan, .et al. , Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
-
glucocorticoid receptor agonist
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.- Sudam S Mane, .et al. , J Am Soc Mass Spectrom, 2024, Aug 26 PMID: 39186802
- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
-
Emodin is a purgative resin, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). It belongs to a family of compounds called anthraquinones, which have shown anti-inflammatory and anticancer effects
- Roberto Brenes, .et al. , J Wildl Dis, 2022, Apr 1;58(2):341-347 PMID: 35255143
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
-
Bcr-Abl inhibitor
Imatinib mesylate, a selective tyrosine kinase inhibitor, induced a sustained objective response in treating gastrointestinal stromal tumors with the inhibition of the KIT signal-transduction pathway.- Inge Govaerts, .et al. , J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. , Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
-
synthetic glucocorticoid receptor agonist
Methylprednisolone is an apoptosis inducer and was also found to inhibit human small cell lung cancer cell growth in vitro. - KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
- Hydroxychloroquine Sulfate 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.
- Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Egawa Y, .et al. , PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
-
glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. -
synthetic glucocorticoid receptor agonist
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent. -
glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
Hepatitis C virus NS3/4a protease inhibitor
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.- Deqiang Kong, .et al. , Nat Commun, 2024, Jun 8;15(1):4894 PMID: 38849338
- Xinyi Wang, .et al. , Nat Chem Biol, 2023, Oct 23 PMID: 37872400
- Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile.
-
glucocorticoid receptor agonist
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent. -
S100A9 inhibitor
Paquinimod is a S100A9 inhibitor, which prevents S100A9 binding to TLR-4. -
RdRp inhibitor
Galidesivir hydrochloride (BCX 4430 hydrochloride) is a viral RNA-dependent RNA polymerase (RdRp) inhibitor; demonstrated broad-spectrum activity in multiple viruses and a favorable preliminary preclinical safety profile. - Artefenomel (OZ439) is a synthetic antimalarial agent with the artemisinin pharmacophore. Artefenomel (OZ439) is a long-acting artemisinin-related agent.
-
broad-spectrum antiviral activity
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. -
synthetic glucocorticoid receptor agonist
Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. -
anti-inflammatory agent
Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. - Merafloxacin, also known as CI 934, is a fluoroquinolone antibacterial, which was also identified as a -1 PRF inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on -1 PRF of other beta coronaviruses. Importantly, frameshift inhibition by merafloxacin substantially impedes SARS-CoV-2 replication in Vero E6 cells, thereby providing the proof of principle of targeting -1 PRF as an effective antiviral strategy for SARS-CoV-2.
- AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
-
SARS-CoV PLpro Inhibitor
4'-O-Methylbavachalcone is a prenylated flavonoid that acts as an inhibitor of the SARS-CoV papain-like protease (PLpro), displaying an IC50 value of 10.1 μM and a Ki of 4.6 μM. This compound has demonstrated the ability to inhibit poly (ADP-ribose) polymerase-mediated cell death and reduce cerebral infarct volume. Additionally, it modulates SUCNR1 activity and interferes with ERK1/2 signaling pathways, affecting cardiomyocyte hypertrophy. 4'-O-Methylbavachalcone is applicable in research focused on ischemic stroke, SARS-CoV, and cardiovascular diseases. -
Anti SARS-CoV-2 Agent
DMA-155 is an antiviral agent that targets SARS-CoV-2 by binding to 5'-terminal stem-loop RNAs, demonstrating affinities of 51.1 μM (SL1), 61.1 μM (SL4), 54.5 μM (SL5a), 66.9 μM (SL5b), and 48.6 μM (SL6). This compound effectively inhibits SARS-CoV-2 viral replication and significantly reduces viral RNA levels. DMA-155 is suitable for research applications related to COVID-19. -
SARS-CoV-2 RdRp Inhibitor
RdRP-IN-10 is a selective inhibitor of the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp), exhibiting an IC50 of 5.78 μM. This compound covalently binds to Cys114 of the SARS-CoV-2 nsp8 protein, disrupting the stabilizing interactions between nsp8 and nsp12. RdRP-IN-10 effectively inhibits RNA polymerization mediated by RdRp without interfering with the RNA-RdRp complex formation. It demonstrates antiviral activity in cellular models and serves as a valuable tool for researching SARS-CoV-2 infection mechanisms and potential therapeutic interventions. -
SARS-CoV-2 Inhibitor
SARS-CoV-2-IN-115 is a potent inhibitor of SARS-CoV-2, demonstrating significant antiviral activity in infected Calu-3 cells with an EC50 of 1.7 μM. This compound effectively inhibits human dihydroorotate dehydrogenase (HsDHODH) with an IC50 of 1.5 μM. Notably, SARS-CoV-2-IN-115 preserves immune response without exhibiting antiproliferative effects on CD4 T cells, making it a valuable tool for research in antiviral therapeutics and immune modulation. -
SARS-CoV-2 Inhibitor
TFMU-ADPr is a selective reporter substrate that targets the SARS-CoV-2 Macro1 protein, displaying an IC50 of 0.59 μM. This compound emits fluorescence at 502 nm (or 495 nm) upon enzymatic hydrolysis by Poly(ADP-ribose) Glycohydrolase (PARG) and ADP-ribosylhydrolase 3. TFMU-ADPr binds to the ADPr-binding site of Macro1, providing a robust method for assessing the activity of poly(ADP-ribose) hydrolases. Its applications extend to evaluating small-molecule inhibitors under in vitro conditions, investigating ADP-ribosyl catabolic enzyme mechanisms, and detecting PAR hydrolase activity in whole-cell lysates, making it a valuable tool for COVID-19-related research. -
SARS-CoV Inhibitor
Direct Violet 1 is an azo dye that functions as an inhibitor of the spike protein-ACE2 interaction in SARS-CoV-2, exhibiting IC50 values ranging from 1.47 to 2.63 μM. This compound serves as a valuable tool for investigating viral entry mechanisms and studying protein-protein interactions related to SARS-CoV-2. Its application may extend to antiviral research and the development of therapeutic strategies targeting COVID-19. -
SARS-CoV-2 Inhibitor
SARS-CoV-2-IN-113 is a sulfonohydrazide derivative designed to inhibit SARS-CoV-2 infection, demonstrating an IC50 of 8.320 μM. This compound exerts significant antiviral activity by blocking viral entry and replication, while also downregulating the expression of key genes and proteins such as Spike, ACE-2, and RdRp. With its high selectivity and low cytotoxicity, SARS-CoV-2-IN-113 serves as a valuable tool for research in the field of SARS-CoV-2 biology and therapeutic development. -
SARS-CoV-2 Inhibitor
SARS-CoV-2 nsp14-IN-3 is an inhibitor of the SARS-CoV-2 N7-Methyltransferase, demonstrating an IC50 value of 3.5 μM. This compound is designed to interfere with the viral methylation process, which is crucial for viral replication and evasion of host immune responses. It serves as a valuable tool in antiviral research and the development of therapeutic strategies targeting SARS-CoV-2. -
SARS-CoV Inhibitor
SARS-CoV-2-IN-7 is a potent inhibitor of the SARS-CoV virus, demonstrating significant antiviral activity with an IC50 value of 844 nM in SARS-CoV-2-infected Vero E6 cells. This compound is primarily utilized in research applications aimed at understanding viral replication processes and developing effective therapeutics against SARS-CoV-2. Its efficacy makes it a valuable tool for studying COVID-19 and potential antiviral strategies. -
SARS-CoV Inhibitor
Bonducellpin D is a furanoditerpenoid lactone that acts as an inhibitor of SARS-CoV and MERS-CoV main proteases (Mpro). With Ki values of 467.11 nM and 284.86 nM for SARS-CoV and MERS-CoV, respectively, it demonstrates broad-spectrum antiviral activity. Additionally, Bonducellpin D exhibits moderate anti-cancer activity in vitro, making it a valuable compound for research into both viral inhibition and cancer therapeutics. -
SARS-CoV Inhibitor
SSAA09E3 is a SARS-CoV entry inhibitor that effectively blocks the entry of SARS/HIV pseudotyped viruses, demonstrating an EC50 of 9.7 μM in 293T cells. Additionally, it has shown significant antiviral activity against SARS-CoV infection in Vero cells, with an EC50 of 0.15 μM. This compound is valuable for research applications aimed at understanding viral entry mechanisms and developing antiviral strategies against SARS-CoV. -
SARS-CoV-2 Inhibitor
AT-9010 triethylamine is a tri-phosphate active metabolite of AT-527 that functions as a potent inhibitor of the NiRAN enzyme, an essential target for viral replication in SARS-CoV-2. It exhibits significant antiviral activity by effectively inhibiting the replication of SARS-CoV-2, making it a valuable tool for research on COVID-19 and potential therapeutic strategies against coronavirus infections. -
SARS-CoV-2 Inhibitor
SARS-CoV-2-IN-15 is a potent inhibitor of SARS-CoV-2, exhibiting an IC50 of 0.49 μM. This niclosamide analogue demonstrates enhanced stability in human plasma and liver S9 enzyme assays compared to its predecessor, which may improve its bioavailability and half-life upon oral administration. SARS-CoV-2-IN-15 is suitable for research applications focused on antiviral drug development and the elucidation of SARS-CoV-2 infection mechanisms. -
SARS-CoV-2 Inhibitor
Cleistanthin B is a potent inhibitor of SARS-CoV-2, demonstrating anti-viral activity with an EC50 of 6.51 µM in Vero cells. This orally active arylnaphthalene lignan lactone glycoside also exhibits notable antitumor, diuretic, and antihypertensive properties in vivo, making it a versatile compound for various research applications in virology and pharmacology. -
SARS-CoV-2 PLpro Inhibitor
GZNL-P36 is a potent inhibitor of SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 6.45 nM, demonstrating effective inhibition of SARS-CoV and its variants with EC50 values ranging from 58.2 nM to 2.66 µM. In pharmacokinetic studies conducted in CD-1 mice, GZNL-P36 achieved a peak plasma concentration (Cmax) of 549 ng/mL, a half-life (T1/2) of 1.45 hours, and a bioavailability of 74.7%. This compound exhibits notable antiviral activity in SARS-CoV-2 XXB.1 infections, positioning it as a valuable tool in therapeutic research against COVID-19. -
SARS-CoV-2 Inhibitor
SARS-CoV-2-IN-78 is an inhibitor of the nsp14 protein of SARS-CoV-2, specifically targeting its N7 methyltransferase activity. This compound demonstrates significant antiviral properties and is valuable for research applications in understanding and mitigating SARS-CoV-2 infection. Its mechanism of action makes it a pertinent tool for studying viral replication and pathogenesis, as well as the development of potential therapeutic strategies against COVID-19. -
SARS-CoV-2 Inhibitor
ZINC000104379474 is a potent inhibitor of SARS-CoV-2 endoribonuclease. It exhibits significant antiviral activity, making it a valuable tool in the study of SARS-CoV-2 replication mechanisms. This compound is particularly relevant for research focused on COVID-19 therapeutics and the development of novel antiviral strategies. -
SARS-CoV-2 Nsp14 Inhibitor
SARS-CoV-2 nsp14-IN-2 is a selective inhibitor of SARS-CoV-2 Nsp14 methyltransferase, exhibiting an IC50 value of 0.093 µM. This compound demonstrates significant antiviral activity and is stable in plasma and liver S9 fractions. SARS-CoV-2 nsp14-IN-2 is valuable for research applications focusing on COVID-19 and the exploration of therapeutic strategies targeting viral replication mechanisms. -
SARS-CoV Inhibitor
SARS-CoV MPro-IN-1 is a covalent inhibitor of the SARS-CoV-2 3CL protease, exhibiting an IC50 of 40 nM. This compound demonstrates significant anti-SARS-CoV-2 activity in cell culture, with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 is suitable for research applications focused on COVID-19 and related viral pathogenesis. -
SARS-CoV-2 Inhibitor
10-Hydroxyaloin A is a potent inhibitor of SARS-CoV-2, specifically targeting the main protease (Mpro) of the virus. This compound demonstrates significant binding affinity to the active site of Mpro, which is crucial for viral replication. 10-Hydroxyaloin A is of particular interest in research applications focused on antiviral drug development and understanding the mechanisms of SARS-CoV-2 inhibition. -
SARS-CoV-2 3CLpro Inhibitor
3CPLro-IN-1 is a potent, orally active inhibitor of the SARS-CoV-2 3CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) plays a critical role in viral replication, making it a significant target for therapeutic intervention against COVID-19. This compound is suitable for research applications focused on developing antiviral strategies and studying the mechanistic pathways of viral replication. -
SARS-CoV-2 Inhibitor
Amb929 is a selective inhibitor targeting the nsp3 protein of SARS-CoV-2, demonstrating significant antiviral activity. It effectively inhibits SARS-CoV-2-mNG replication in VeroE6 cells with an EC50 of 34.7 µM and has a moderate cytotoxicity profile, with a CC50 of 281 µM. Additionally, Amb929 shows effectiveness in suppressing viral replication in Human Airway Epithelium (HAE) models, making it a valuable tool for research on COVID-19 and therapeutic development.

