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].
Nafcillin sodium is a second generation penicillinase-resistant penicillin antibiotic. Nafcillin sodium can be used for the research of staphylococcal infections[1][2][3].
Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase (AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity[1][2].
Ac-dA Phosphoramidite is a phosphinamide monomer that can be used in the preparation of oligonucleotides.
Sulfapyridine D4 a deuterium labeled Sulfapyridine. Sulfapyridine is a sulfonamide antibacterial[1].
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].
Toremifene-d6 (Z-Toremifene-d6) citrate is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
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.
Niclosamide is an inhibitor of STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
2-Keto-D-Glucose (D-Glucosone) is a key intermediate in a secondary metabolic pathway leading to the antibiotic Cortalcerone. 2-Keto-D-Glucose is also an intermediate in the conversion of D-glucose into D-fructose. 2-Keto-D-Glucose is found in various natural sources, including fungi, algae, and shellfish[1][2].
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.
Isoleucyl tRNA synthetase-IN-1 (compound 11) is a potent and selective isoleucyl-tRNA synthetase (IleRS) inhibitor, with a Ki,app of 88 nM[1].
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.
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].
T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
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].
Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani[1].
Tectoquinone (2-Methylanthraquinone) is a SARSCoV-2 main protease inhibitor against COVID-19. Tectoquinone exhibits strong mosquito larvicidal activity with the LC50 values of 3.3 and 5.4 μg/ml against A. aegypti and A. albopictus in 24 h, respectively[1][2].
3,6-Dichlorocatechol is a substrate of the broad-spectrum chlorocatechol 1,2-dioxygenase of pseudomonas chlororaphis RW71[1].
Isoeuphorbetin, a dimeric coumarin isolated from Viola philippica, is a potent HCV protease inhibitor with an IC50 of 3.63 µg/mL[1].
T-705RTP sodium is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP sodium is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity[1][2].