NBD-14189 is a potent HIV-1 entry antagonist with an IC50 of 89 nM against the HIV-1HXB2 pseudovirus. NBD-14189 binds to HIV-1 gp120 and shows potent antiviral activity (EC50<200 nM)[1][2].
HBV-IN-6 is a potent HBV inhibitor with an EC50 of 44 nM (WO2021213445A1, compound 3)[1].
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth[1][2].
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity[3][4].
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits Autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1[1][2][3][4].
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacterium tuberculosis (Mtb), without cytotoxicity. Mtb-IN-2 significantly decreases colony-forming units (CFU) in spleen of murine tuberculosis models, and distinguishes both drug-sensitive and drug-resistant Mtb H37Rv strains. Mtb-IN-2 affects methionine metabolism but not folate pathway directly.
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 µM and 1.4 µM for Trypanosoma brucei (TB) and human CYP51, respectively[1].
Sulfamethizole is a sulfathiazole antibacterial agent.Target: AntibacterialSulfamethizole is a sulfathiazole antibacterial agent. Sulfamethizole is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid. Sulfamethizole, an inhibitor of dihydropteroate synthetase and the formation of folic acid, inhibited bioluminescence more than growth [1]. Treatment with sulfamethizole resulted in a significant reduction in bacterial counts in all samples from a susceptible strain (MIC, 128 micro g/ml) and a resistant strain (MIC, 512 micro g/ml). Infection with a sulII gene-positive strain (MIC, >2,048 micro g/ml) could not be treated with sulfamethizole, as no effect could be demonstrated in the urine, bladder, or kidneys [2].
Pradofloxacin, a third-generation fluoroquinolone antibacterial agent[1]
Agathisflavone is a flavonoid with antioxidant, anti-inflammatory, antiviral, antiparasitic, cytotoxic, neuroprotective, and hepatoprotective activities. Agathisflavone can improve tissue repair in a spinal cord injury model in rats[1][2][3].
HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC50 value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS[1].
Tropesin (VUFB 12018; Repanidal) is a nonsteroid antiinflammatory agent (NSAIA) that inhibits the growth of Trichoderma viride[1].
TCMDC-125457 is potent in inducing calcium redistribution but minimally inhibits heme crystallization. TCMDC-125457 demonstrated high efficacy when pulsed in a single-dose combination with artesunate against tightly synchronized artemisinin-resistant ring-stage parasites.
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine[1]. 2'-Deoxy-2'-fluorouridine can be used as an intermediate for antiinfluenza virus agents synthesis[2].
NS2B/NS3-IN-3 hydrochlorideis an inhibitor of Flavivirus NS2B-NS3 protease[1].
MsbA inhibitor 1 is a novel small molecule lipopolysaccharide biogenesis inhibitor, inhibits MsbA, an ATP-dependent flippase that translocates LPS across the inner membrane; causes mislocalization of LPS to the cell interior, inhibits Δ5 strain with MIC of 0.2 ug/ml.
Neotripterifordin is a inhibitor of HIV. Neotripterifordin has anti-HIV replication activity in H9 lymphocyte cells with an EC50 of 25 nM[1].
Dasabuvir (ABT-333) is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the HCV NS5B gene, inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC50 between 2.2 and 10.7 nM.
Lopinavir Metabolite M-1, an active metabolite of Lopinavir, inhibits HIV protease with a Ki of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro[1][2].
Olaquindox, a quinoxalin derivative, is an orally active antibiotic veterinary drug. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets[1].
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species[1].
Olgotrelvir is an antiviral agent[1].
Polyphyllin C (compound 2) is a spirostanol saponin. Polyphyllin C exhibits mild (IC50=36.87 µM) activities against the tyrosinase and moderate (IC50=1.59 µg/mL) antileishmanial activities[1][2].
Methicillin-d6 sodium salt is the deuterium labeled Methicillin sodium salt. Methicillin sodium salt is a β-lactam antibiotic which acts by inhibiting penicillin-binding proteins that are involved in the synthesis of peptidoglycan.
Licorice glycoside C2 is a oleanane-type triterpene oligoglycoside isolated from Glycyrrhiza uralensis. Various biological activities are associated with licorice extracts, such as anti-viral, anti-microbial, antioxidant, anti-inflammatory, anti-ulcer, anti-cancer and anti-HIV effects[1].
Ocotillone ((24S)-20,24-Epoxy-25-hydroxydammaran-3-one) is a triterpenoids that can be isolated from the fruits of Dysoxylum richii. Ocotillone has antibacterial activities against P. aeruginosa and S. typhimurium without hemolytic activity[1].
Amiprilose (SM1213; Therafectin) is a potent inhibitor against Hepatocellular carcinoma (HCC). Amiprilose induces lymphokine-induced macrophage activation directly to kill Listeria monocytogenes[1][2].
Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic.Target: AntibacterialSulfonamides are structural analogs and competitive antagonists of para-aminobenzoic acid (PABA). They inhibit normal bacterial utilization of PABA for the synthesis of folic acid, an important metabolite in DNA synthesis. The effects seen are usually bacteriostatic in nature. Folic acid is not synthesized in humans, but is instead a dietary requirement. This allows for the selective toxicity to bacterial cells (or any cell dependent on synthesizing folic acid) over human cells. Bacterial resistance to sulfamethoxazole is caused by mutations in the enzymes involved in folic acid synthesis that prevent the drug from binding to it.
N-(Ketocaproyl)-D,L-homoserine lactone is a natural, very active ligand of LuxR. N-(Ketocaproyl)-D,L-homoserine lactone is a quorum sensing (QS) autoinducer[1].
PI-55 is a specific cytokinin receptor inhibitor. PI-55 is structurally related to 6-benzylaminopurine (BAP) and was shown to inhibit competitively BAP binding on Arabidopsis-specific receptors CRE1/AHK4 and AHK3. PI-55 inhibits cytokinins induced haustorium formation and increased parasite aggressiveness[1].