Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines [1][2].
Debneyol exhibits more potent fungicidal activity than validamycin.
Doramectin is an antiparasitic agent.IC50 Value:Target: AntiparasiticDoramectin (Dectomax) is a veterinary drug approved by the Food and Drug Administration (FDA) for the treatment of parasites such as gastrointestinal roundworms, lungworms, eyeworms, grubs, sucking lice and mange mites in cattle. Mutational biosynthetic antiparasitic antibiotic structurally related to the avermectins.
Ro 24-4383 is a carbamate-linked dual action antibacterial agent[1].
Boceprevir is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.
Mesoxalate (Ketomalonic acid) a dicarboxylic acid and a ketonic acid which blocks HIV-1 reverse transcriptase (RT), with the IC50 of 2.2 μM[1][2].
Tanshinlactone is a seco-abietanoid that can be isolated from Salvia miltiorrhiza. Tanshinlactone is a coronavirus (CoV) inhibitor. Tanshinlactone modulates interleukin-2 and interferon-γ gene expression[1][2].
Maftivimab (REGN3470-3471-3479), the inhibitor of Filovirus, is an Food and Drug Administration (FDA)-approved agent. Maftivimab, also named as Atoltivimab, Odesivimab (Inmazeb), can be used for research of Zaire ebolavirus infection[1].
RSV/IAV-IN-2 (compound 14c) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-2 has lesser cytotoxicity than the clinical drug, Ribavirin. RSV/IAV-IN-2 has the potential for the research of RSV and/or IAV infections[1].
Antibacterial agent 98 (compound g37) is a potent and orally active antibacterial agent. Antibacterial agent 98 inhibits the ATPase activity of Gyrase B and impairs Staphylococcus aureus (S. aureus ) DNA supercoiling. Antibacterial agent 98 shows antibacterial activity and not induce resistance development of MRSA (methicillin-resistant S. aureus)[1].
DENV-IN-5 (Compound 4b) is a dengue virus (DENV) inhibitor with EC50s of 1.47, 9.23, 7.08 and 8.91 μM against DENV-I ∼ IV replication, respectively. DENV-IN-5 also inhibits HIV-1IIIB strain with an EC50 of 0.1512 μM[1].
Proflavine (3,6-Diaminoacridine) dihydrochloride, an acridine dye, is a DNA intercalating agent and Anti-microbial agent. Proflavine dihydrochloride behaves as a pore blocker for Kir3.2. Proflavine dihydrochloride is a potential lead compound for Kir3.2-associated neurological diseases[1][2][3].
Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase (AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity[1][2].
Sulfapyridine D4 a deuterium labeled Sulfapyridine. Sulfapyridine is a sulfonamide antibacterial[1].
2-Deoxy-D-glucose-d1 is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
Cefaloglycin (Cephaloglycin) is an orally active nephrotoxic β-lactam cephalosporin antibiotic with antibacterial activity. Cefaloglycin is activity against Gram-Positive cocci other than enterococci. Cefaloglycin is toxic to mitochondrial substrate uptake and respiration[1][2][3].
Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects.
Abafungin, a antifungal agent, inhibitis the transmethylation at the C-24 position of the sterol side chain, catalyzed by the enzyme sterol-C-24-methyltransferase.
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.IC50 Value: 0.94 μM (HCV NS5B 1a); 1.2 μM (HCV NS5B 1b)Target: HCVVX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection. VX-222 exhibits non-competitive and selective inhibition in HCV NS5B of genotype 1a and 1b, with IC50 of 0.94 and 1.2 μM, respectively. VX-222 selectively inhibits the replication of subgenomic HCV genotype 1a and 1b with an EC50 of 22.3 and 11.2 nM, respectively. [1] Similarly, a recent study shows that VX-222 inhibits the 1b/Con1 HCV subgenomic replicon, with an EC50 of 5 nM. In rats and dogs, VCH-222 displays fine pharmacokinetic pro le, including low total body clearance and excellent oral bioavailability (greater than 30%) and good ADME properties. VCH-222 is biotransformed by several enzymes (CYP1A1, 2A6, 2B6, 2C8, CYP 3A4, UGT1A3) and is predicted to be actively transported in liver and excreted mainly intact in bile or as glucuronide adducts.
Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. Nacubactam (OP0595 free acid) acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs[1][2].
Ethopabate is an antiprotozoal agent which has been widely used to treat and prevent coccidiosis in chickens.
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.
Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics, with activity similar to oxolinic acid and nalidixic acid.
Primin is a natural product stored in trichomes on leaves and stems of Primula obconica, with antimicrobial and antitumour properties[1][2].
Valnivudine (FV-100 free base), a prodrug of CF-1743, is an orally active anti-herpes zoster (HZ) nucleoside analogue. CF-1743, a bicyclic nucleoside analog (BCNA), has highly specific antiviral activity against varicella-zoster virus (VZV). Valnivudine is rapidly and extensively converted to CF-1743 in vivo[1][2].
InhA-IN-4 (TU14) is a Mycobacterium tuberculosis InhA (an enoyl ACP-reductase) inhibitor with an IC50 of 15.6 μM[1].
ASP2397 (VL-2397), a natural compound, exhibits rapid and potent fungicidal activity against Aspergillus species, at a MIC range of 1 to 4 μg/mL in human serum. ASP2397 (VL-2397) has the potential to treat invasive pulmonary aspergillosis (IPA)[1].
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase[1][2][3].
Enterocin K1 (EntK1) is a bacteriocin. Enterocin K1 is a ribosomal synthetic peptide. Enterocin K1 specifically targets Enterococcus faecalis via the Eep protein on the bacterial membrane. Enterocin K1 displays a potent antibacterial activity against VRE. Enterocin K1 can be used for related studies of VRE infections[1].