L-Lysine-13C dihydrochloride is the 13C-labeled L-Lysine dihydrochloride. L-lysine dihydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.

Phleomycin D1 (PLM D1), a glycopeptide antibiotic, is a member of the Bleomycin/Phleomycin family. Phleomycin D1 causes cell death by binding and cleaving DNA.

Ticlatone is an antifungal that can be used for the research of mycoses.

1-Phenylsemicarbazide is an antifungal agent. 1-Phenylsemicarbazide has the potential for preventing mold growth on industrial products.

(S)-1-(4-Hydroxyphenyl)ethane-1,2-diol is an active constituent of the aerial parts of Angelica sinensis. (S)-1-(4-Hydroxyphenyl)ethane-1,2-diol significantly inhibits the growth of Aeromonas hydrophila. Anticoagulative and antibiotic activities.

Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity.

Indolicidin acetate is a potent antimicrobial peptide purified from the cytoplasmic granules of bovine neutrophils.

TNP-2198 is a potent and orally bioavailable dual-targeted antibacterial agent. TNP-2198 has potent activity against microaerophilic and anaerobic bacterial pathogens.

Antibacterial agent 68 (compound 4d) is an antibacterial agent against drug-resistant Escherichia coli. Antibacterial agent 68 has low cytotoxicity and exerts strong antibacterial activities against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM.

MsbA-IN-2 (compound 12) is a potent lipopolysaccharide transporter MsbA inhibitor with an IC50 of 2 nM for E. coli MsbA.

17-Hydroxyventuricidin A (YP-02259L-C) is an antimicrobial compound.17-Hydroxyventuricidin A inhibits the growth of the two tested filamentous fungi (Verticillium dahlia and Fusarium sp.) and of Candida tropicalis R2 CIP203.

Sulfadiazine-13C6 is a labeled Sulfadiazine. Sulfadiazine is a sulfonamide antibiotic with antimalarial activity.

Desfuroylceftiofur is an active metabolite of Ceftiofur which is a broad-spectrum cephalosporin antibiotic. Desfuroylceftiofur is active against gram-positive and gram-negative bacteria.

Octanal is an aromatic aldehyde, with antioxidant and antimicrobial activities. Octanal shows cytotoxicity against Hela cells.

Curvulamine A, an antibacterial alkaloid, shows potent antibacterial activity.

2-Hydroxydocosanoic acid has antioxidant, cholinesterase inhibitory, and antimicrobial activities.

RmlA-IN-1 (Compound 8a) is a potent inhibitor of glucose-1-phosphate thymidylyltransferase (RmlA) with an IC50 of 0.073 μM. RmlA-IN-1 influences monosaccharide l-Rhamnose biosynthetic pathway. RmlA-IN-1 affects bacterial cell wall permeability.

Penicolinate A is a picolinic acid derivative. Penicolinate A is isolated from endophytic Penicillium sp. BCC16054. Penicolinate A exhibits antimalarial and antitubercular activities.

FPI-1465 acts a dual inhibitor of serine-β-Lactamases and Penicillin-binding proteins (PBPs).FPI-1465 inhibits PBP2 (IC50=1.0 µg/mL). FPI-1465 exhibits activity against β-lactamase CTX-M-15 and OXA-48 with Kds of 0.011 and 5.3 µM, respectively.

Afabicin (Debio 1450) is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.

Antibacterial agent 74 (compound 36) is an anti-Salmonella agent.

Talaromycesone A is an oxaphenalenone dimer compound. Talaromycesone A exhibits potent antibacterial activities with an IC50 of 3.70 μM, against human pathogenic Staphylococcus strains. Talaromycesone A displays potent acetylcholinesterase inhibitory activities with an IC50 of 7.49 μM.

Kumbicin C is a bis-indolyl benzenoid compound from an Australian soil fungus, Aspergillus kumbius. Kumbicin C inhibits the growth of mouse myeloma cells and the Gram-positive bacterium Bacillus subtilis.

Anticancer agent 34 (compound 9), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 34 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/ml. Anticancer agent 34 inhibits A549, PC3 cell growth with IC50s of 8.4 µg/ml, 7.8 µg/ml, respectively.

Pachybasin is a major metabolite from culture broth of endophytic coelomyceteous AFKR-18 fungus. Pachybasin showes antimicrobial activities against E. coli, B. subtilis, M. luteus, S. cerevisiae, C. albicans, A. niger, and A. flavus, with MIC values of 64.0 μg/mL, and against S. aureus and F. oxysporum with MIC values of 32.0 and 16.0 μg/mL respectively.

epi-Equisetin, a secondary metabolite, has antibacterial activity.

c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively.

c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively.

Monocerin is an isocoumarin derivative. Monocerin is isolated from Microdochium bolleyi, an endophytic fungus from Fagonia cretica. Monocerin shows good antifungal, antibacterial, and antialgal activities against Microbotryum violaceum, Escherichia coli, Bacillus megaterium, and Chlorella fusca.

Poly(hexamethylenebiguanide) hydrochloride is an antimicrobial agent, which can be used in medical, apparel, and household textile sectors.

4-Piperidinecarboxamide is a mycobacterial aspartyl-tRNA synthetase (AspS) inhibitor. 4-Piperidinecarboxamide is a promising anti-tuberculosis (TB) agent.

Antibacterial agent 64 is a potent YycG inhibitor (IC50=6.1 µM) and an antibacterial agent. Antibacterial agent 64 combines with ampicillin could synergistically eradicate the biofilm-embedded viable bacteria.

Radicinol is a metabolite of cochliobolus lunata, and absolute stereochemistry of radicinin.

Antibacterial agent 27 is a potent antibacterial compound against Candida species.

Antibacterial agent 26 is a potent antibacterial compound.

Sulfisoxazole acetyl (N1-Acetylsulfisoxazole), a Sulfisoxazole derivative, is an orally active dihydropteroate synthase inhibitor. Sulfisoxazole acetyl has an antibacterial action.

DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both drug-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs<0.1 μg/mL, as well as good intracellular antimycobacterial activity with a 1.29 log10 CFU reduction in macrophages.

Anticancer agent 36 (compound 11), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 36 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/L. Anticancer agent 36 inhibits A549, PC3 cell growth with IC50s of 19.7 µg/mL, 11.9 µg/mL, respectively.

Antibacterial agent 75 (compound 24) is an antibacterial agent. Antibacterial agent 75 (compound 24) is able to re-sensitize VRSA to vancomycin.

Antibacterial agent 82 (compound 7p) is an antibacterial agent.

Antibacterial agent 76 (compound 9) is an antibacterial agent.

Antibacterial agent 77 (compound 12) is an antibacterial agent.

Antibacterial agent 79 (compound 32) is an antibacterial agent.

Antibacterial agent 80 (compound 20) is an antibacterial agent.

RmlA-IN-2 (Compound 1d) is a potent inhibitor of glucose-1-phosphate thymidylyltransferase (RmlA) with an IC50 of 0.303 μM. RmlA-IN-2 influences monosaccharide l-Rhamnose biosynthetic pathway. RmlA-IN-2 affects bacterial cell wall permeability.

Sulfaguanidine-d4 is the deuterium labeled Sulfaguanidine. Sulfaguanidine, belongs to the class of sulfonamide drug, is an orally active antibiotic. Sulfaguanidine can be used for the research of enteric infections such as bacillary dysentery.

Amp1EP9 is an antimicrobial peptide. Amp1EP9 is a powerful tool for developing potent and nontoxic antimicrobial drugs. Amp1EP9 has the potential for the research of multidrug-resistant bacterial infections.

Antibacterial agent 78 (compound 30) is an antibacterial agent.

Ph-Ph+ is a hemiprotonic compound, which is produced from phenanthroline (ph) dimerization. Ph-Ph+ has antitumor, antibacterial and antifungal activities.

DMA-135 hydrochloride inhibits enterovirus 71 (EV71) IRES-dependent translation and replication. DMA-135 hydrochloride binds to enterovirus 71 (EV71) SLII domain with moderately high affinity (KD= 520 nM). DMA-135 hydrochloride has no significant toxicity in cell-based studies.

EV-A71-IN-1 is a human enterovirus A71 (EV-A71) capsid protein inhibitor with an EC50 of 0.27 μM against EV-A71. EV-A71-IN-1 is a capsid binder that blocks the interaction between the viral VP1 and the host receptor hSCARB2. EV-A71-IN-1 inhibits a series of different human enteroviruses without significant cytotoxicity (CC50>56.2 μM).

N'-(2-Fluorophenyl)pyrazine-2-carbohydrazide is a Ole1p desaturase inhibitor and antifungal agent.

Cladospirone bisepoxide is a metabolite that isolated from cultures of a fungus. Cladospirone bisepoxide displays selective antibiotic activity against several bacteria and fungi and inhibits germinations of Lepidium sativum at low concentrations.

Harzianum A is a trichothecene that isolated from the soil-borne fungus Trichoderma harzianum. Harzianum A shows no cytotoxicity against baby hamster kidney cells, no activity against Gram-negative and Gram-positive bacteria, but modest antifungal activity at 100 μg/mL.

Viridiol, a fungal metabolite from Trichodernza viride, shows antifungal activity.

CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis.

FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC80 of 1 μg/mL.

SDH-IN-1 (compound 4i) is a succinate dehydrogenase (SDH) inhibitor with an IC50 of 4.53 μM. SDH-IN-1 has potent antifungal activities. SDH-IN-1 displays potent activity against S. sclerotiorum (EC50 of 0.14 mg/L).

BI-10 is an antifungal compound. BI-10 combined with Fluconazole can inhibit hyphal growth, result in ROS accumulation, and decrease mitochondrial membrane potential (MMP) as well as altering membrane permeability.

1233B is a secondary metabolite from filamentous fungus, Fusarium sp. RK97-94.

Bis(methylthio)gliotoxin is a more stable and reliable marker for invasive aspergillosis than gliotoxin and suitable for use in diagnosis.

Globosuxanthone A is a dihydroxanthenone with obvious antifungal activity towards Fusarium graminearum, Fusarium solani, and Botrytis cinerea with MIC values of 4, 8, and 16 μg/mL, respectively. Anticancer activity.

Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor (IC50=0.12 mM). Chitin synthase inhibitor 1 has potent antifungal activity against drug-resistant fungi variants.

BA38017 is a potent HBV core protein assembly modulator. BA38017 inhibits HBV replication with an EC50 of 0.20 μM.

HBV-IN-17 (compound 8) is a potent HBV capsid assembly modulator with an EC50 of 511 nM.

SHR5133 is a highly potent, orally active HBV capsid assembly modulator. SHR5133 displays HBV DNA reduction (EC50=26.6 nM).

HBV-IN-16 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-16 is a quinoline derivative. HBV-IN-16 has the potential for the research of HBV infection (extracted from patent WO2019121357A1, compound 1).

HBV-IN-14 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-14 is a pyridinopyrimidinones compound. HBV-IN-14 has the potential for the research of HBV infection (extracted from patent WO2021190502A1, compound 5).

GSK8175 is a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV). GSK8175 is a sulfonamide- N-benzoxaborole analog with low in vivo clearance across preclinical species and broad-spectrum activity against HCV replicons.

UK-1 is a cytotoxic metabolite from Streptomyces sp. 517-02 and exerts a wide spectrum of potent anticancer activities. UK-1 also inhibits HCV replication.

AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection.

Guanosine-8-d is a deuterium labeled Guanosine. Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity.

Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28).

Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1).

Cap-dependent endonuclease-IN-26 is a cap-dependent endonuclease (CEN) inhibitor with an IC50 of 286 nM. Cap-dependent endonuclease-IN-26 shows antiviral activity against many influenza A and B strains.

Cap-dependent endonuclease-IN-3 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-3 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-3 has the potential for the research of influenza A and influenza B infection (extracted from patent WO2019141179A1, compound VI-1).

Cap-dependent endonuclease-IN-25 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-25 is a macrocyclic pyridotriazine derivative. Cap-dependent endonuclease-IN-25 has the potential for the research of viral infections caused by viruses belonging to the Orthomyxoviridae family (extracted from patent WO2020075080A1, compound 4).

Cap-dependent endonuclease-IN-5 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-5 inhibits influenza virus well, and/or has lower cytotoxicity, better in vivo pharmacokinetic properties and in vivo pharmacodynamic properties (extracted from patent WO2020078401A1, compound 13-1).

Cap-dependent endonuclease-IN-8 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-8 inhibits replication of orthomyxoviruses (including influenza A, influenza B and influenza C) (extracted from patent CN111410661A, compound I-196).

Cap-dependent endonuclease-IN-12 (EXP-35) is a potent Cap-dependent endonuclease inhibitor with low cytotoxicity. Cap-dependent endonuclease-IN-12 shows inhibitory activity against H1N1.

Neuraminidase-IN-5 (Compound 5b) is a potent inhibitor of neuraminidase with an IC50 of 0.02 μM. Neuraminidase (NA) is a promising target for development of anti-influenza drugs. Neuraminidase-IN-5 is a dihydrofurocoumarin derivative compound.

Cap-dependent endonuclease-IN-7 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-7 Inhibits the synthesis of viral mRNA and eventually inhibits virus proliferation. Cap-dependent endonuclease-IN-7 has the potential for the research of viral infections (including influenza A, influenza B and influenza C) (extracted from patent WO2020177715A1, compound 5)

Cap-dependent endonuclease-IN-6 (compound 13) is a cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-6 shows inhibition against influenza virus (EC50=38.21 nM).

Cap-dependent endonuclease-IN-19 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-19 is a spirocyclic pyridone derivative. Cap-dependent endonuclease-IN-19 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN111410661A, compound 1).

Cap-dependent endonuclease-IN-15 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-15 inhibits the replication of influenza virus. Cap-dependent endonuclease-IN-15 has the potential for the research of viral infections caused by influenza viruses (extracted from patent CN113226327A, compound c-1).

Cap-dependent endonuclease-IN-22 is a potent cap-dependent endonuclease (CEN) inhibitor.

Cap-dependent endonuclease-IN-16 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-16 is a pyridone polycyclic derivative. Cap-dependent endonuclease-IN-16 has the potential for the research of influenza (extracted from patent CN112778330A, compound 15A).

Cap-dependent endonuclease-IN-24 is a potent cap-dependent endonuclease (CEN) inhibitor (CN112876510A, DSC1103).

Cap-dependent endonuclease-IN-17 is a cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-17 shows antiviral activity against influenza virus A/Hanfang/359/95 (H3N2) with IC50 of 1.29 μM (CN112898346A; DSC701).

Cap-dependent endonuclease-IN-18 is a potent cap-dependent endonuclease (CEN) inhibitor (CN112898312A, compound 14).

Cap-dependent endonuclease-IN-20 is a cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-20 shows antiviral activity against influenza virus A/Hanfang/359/95 (H3N2) with IC50 of 4.82 μM (CN112940009A; DSC801).

Cap-dependent endonuclease-IN-11 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-11 has the potential for the research of viral infections (extracted from patent WO2021129602A1, compound DSC126).

Cap-dependent endonuclease-IN-10 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-10 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo pharmacokinetic and in vivo pharmacodynamic properties, and better hepatic microsomal stability. Cap-dependent endonuclease-IN-10 has the potential for the research of viral infections (including influenza A, influenza B and influenza C) (extracted from patent WO2021129799A1, compound 1-1).

Neuraminidase-IN-3 (compound 23d) is a potent influenza neuraminidase (NA) inhibitor with IC50 values of 0.73, 0.26, and 0.63 nM against H1N1, H5N1, and H5N8 NAs, respectively.

Cap-dependent endonuclease-IN-13 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-13 has the potential for the research of influenza virus infection (only influenza A) (extracted from patent WO2021180147A1, compound I-1).

Neuraminidase-IN-6 (Compound 5c) is a potent inhibitor of neuraminidase with an IC50 of 0.11 μM. Neuraminidase-IN-6 is a 1,3,4-triazole-3-acetamide derivative. Neuraminidase (NA) is an ideal target for the development of anti-influenza drugs.

Cap-dependent endonuclease-IN-14 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-14 inhibits the replication of influenza virus. Cap-dependent endonuclease-IN-14 has the potential for the research of viral infections caused by influenza viruses (extracted from patent CN113620948A, compound 1-c).

Cap-dependent endonuclease-IN-21 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-21 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-21 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8B or 8A).

Cap-dependent endonuclease-IN-23 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-23 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-23 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8A or 8B).

Herquline A (Herqueline A) is a fungal piperazine alkaloid. Herquline A is a fungal metabolite that inhibits platelet aggregation and replication of the influenza virus.

Neuraminidase-IN-4 (Compound 4b) is a potent inhibitor of neuraminidase with an EC50 of 1.59 μM. Neuraminidase (NA) is an important target for the treatment of influenza. Neuraminidase-IN-4 exhibits excellent antiviral activity against A/chicken/Hubei/327/2004 (H5N1-DW).

Cycloaspeptide A, isolated from the endophytic fungus Penicillium janczewskii, has antiparasitic activity.

Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human.

CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively).

HDAC1-IN-4 (JX34) is a potent Plasmodium falciparum HDAC1 inhibitor shows antimalarial activity (IC50 < 5 nM) and lower cytotoxicity.

Antimalarial agent 10 (Compound 17b) is an aminoalcohol quinoline compound. Antimalarial agent 10 is an antimalarial agent with IC50 values of 14.9 nM and 11.0 nM against respectively Pf3D7 and PfW2 and a selectivity index higher than 770 whatever the cell line is.

Antiviral agent 15 (Compound 15f) is a Clofazimine derivative with antiviral effects. Antiviral agent 15 inhibits both rabies virus and pseudo-typed SARS-CoV-2 with EC50 values of 1.45 μM and 14.6 μM, respectively.

αGalCer-RBD is a self-adjuvanting lipoprotein conjugate. αGalCer-RBD induces potent immunity against SARS-CoV-2 and its variants of concern. αGalCer-RBD conjugate induces RBD-specific, cytokine-producing T cell development. αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate. α-Galactosylceramide (αGalCer) is a potent invariant natural killer T cell (iNKT) agonist. RBD: receptor-binding domain

Sulfamethoxazole-13C6 is a 13C labeled Sulfamethoxazole. Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonist of para-aminobenzoic acid (PABA).

ient S. Tm and hyperpermeable Escherichia coli. The potencies against WT strains of E. coli, Acinetobacter baumannii, and Burkholderia cenocepacia are also improved considerably (up to >128-fold) with the outer-membrane permeabi

Parabulin is a novel potent, parasite-specific tubulin inhibitor, inhibits growth of parasites while displaying no effects on human cells.

GSK-2485852 (GSK2485852, GSK5852) is a highly potent, selective HCV NS5B polymerase inhibitor with IC50 of 3.0 and 1.6 nM for HCV genotypes 1a and 1b in replicon assay, respectively.

GSK-2878175 (GSK8175, GSK-175, GSK-175A) is a potent, pan-genotypic, second generation HCV NS5B palm polymerase inhibitor with EC50 of 0.4-9.7 nM.

GSK 3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).

MEDS433 is a potent DHODH inhibitor with IC50 of 1.2 nM (hDHODH), inhibits in vitro replication of HSV-1 and HSV-2 in the nanomolar range.

INE963 (INE-963) is a potent and fast-acting blood-stage antimalarial, demonstrates potent cellular activity against Pf 3D7 with EC50 of 6 nM in Pf growth inhibition assay.

1-ECBC is a small molecule inhibiting C. albicans filamentation, 1-ABC targets DYRK1-family kinase Yak1, the sole DYRK-family member expressed in C. albicans.1-ECBC blocked C. albicans biofilm formation in several co-culture models and a rat catheter infection model.

2S-alkyne is an irreversible and clickable inhibitor of Streptococcal pyrogenic exotoxin B (SpeB) with IC50 of 1.4 uM; 2S-alkyne showed irreversible enzyme inhibition in biochemical assays and labeled endogenous SpeB in cultured S. pyogenes supernatants. 2S-alkyne decreased S. pyogenes survival in the presence of human neutrophils and supports the role of SpeB-mediated proteolysis as a mechanism to limit complement-mediated host defense.

90 (CBR-490) is a potent and selective antiwolbachial activity compound (Anti-Wolbachia wMel In vitro HCI cell-based assay IC50=33 nM, IC90=283 nM).CBR490 demonstrates potent antiwolbachial activity was confirmed in L. sigmodontis, Brugia malayi, and Onchocerca ochengi in vivo preclinical models of filarial disease.CBR490 demonbstrated in vitro selectivity against Loa loa (a safety concern in endemic areas).

A highly potent, selective HCV NS5B polymerase inhibitor for treatment of HCV infection.

A small molecule CD4-mimetic that binds gp120 and blocks CD4 binding, inhibits HIV-1 entry.

AB-452 (AB452) is a potent, small molecule inhibitor of noncanonical poly(A) polymerases PAPD5 and PAPD7 (PAPD5/7), inhibits PAPD5/7 enzymatic activities, reduces HBsAg in vitro (EC50=1.4/6.8 nM).AB-452 demonstrated specific antiviral activity for HBV, was inactive against a panel of 10 different RNA and DNA viruses with EC50 values of >30 uM.AB-452 reduced HBsAg, HBeAg, and HBV DNA production with EC50 of 0.28-6.8 nM, without cytotoxicity.AB-452 interferes with multiple steps of HBV life cycle by reducing HBV RNA.AB-452 demonstrated antiviral activity in AAV-HBV-transduced mouse model.AB-452 promotes HBV RNA degradation through inhibiting PAPD5 and PAPD7 enzymatic activities and blockage of guanosine incorporation into viral RNA poly(A) tails..

AB-506 is a small-molecule inhibitor targeting HBV core protein, inhibits viral replication in vitro (IC50=77 nM).AB-506 binds to HBV core protein, accelerates capsid assembly and inhibits HBV pgRNA encapsidation.AB-506 blocks cccDNA establishment in HBV-infected HepG2-hNTCP-C4 cells and primary human hepatocytes, leading to inhibition of viral RNA, HBsAg, and HBeAg production (EC50=0.64-1.52 uM).AB-506 demonstrated activity across HBV genotypes A-H and maintains antiviral activity against nucleostide analog-resistant variants in vitro.AB-506 showed an 8 to 20-fold increase in EC50 values against L30F, L37Q, and I105T substitutions.AB-506 exhibits good oral bioavailability, systemic exposure, and higher liver to plasma ratios in rodents.

ACAi-028 is a small molecule inhibiting HIV-1 replication (EC50=0.55 uM) that targets a hydrophobic pocket in the N-terminal domain of capsid (CA-NTD).ACAi-028 binds directly and noncovalently to HIV-1 capsid monomer.ACAi-028 inhibits the early stage of the HIV-1 life cycle and does not affect the late stage, also prevents multiple-round HIV-1 infection using HIV-1 strains (HIV-1NL4-3 and HIV-1LAI), except for HIV-2 strain (HIV-2ROD).ACAi-028 inhibits the replication of various types of HIV-1 strains (HIV-1104pre and HIV-1MDR/B) in PBMCs and HIV-1ATVR5μM in MT-4 cells, with negligible cytotoxicity.

ACHN-975 (ACHN975) is a potent bacterial LpxC inhibitor with IC50 of 0.68 nM (P. aeruginosa LpxC); ACHN-975 is potent against the P. aeruginosa isolates with MIC50 of 0.06 ug/mL and MIC90 of 0.25 ug/mL. ACHN-975 demonstrated in a neutropenic mouse thigh model with P. aeruginosa ATCC 27853.

Amphihevir is a potent, selective HCV NS4B inhibitor with EC50 of 0.34 and 1.97 nM against the GT1a (H77) and GT1b replicon in luciferase assays.Amphihevir shows weaker acitivity against GT2a (JFH-1) (EC50=186 nM).Amphihevir shows EC50 3.13 nM and 18.16 nM with 100% human serum against GT1a and GT1b replicons using HCV-1b replicon cells test.Amphihevir reduced replicon RNA by nearly 6,300-fold (3.8 log10) at a concentration 25-fold greater than the EC90 (300 nM).Amphihevir was found to be inactive against other viruses, human kinases, and GPCRs, which implies its good selectivity.Amphihevir has good oral bioavailability and appropriate T1/2 in rats and dogs, showed good safety profiles in rats and dogs.Amphihevir is the first reported NS4B inhibitor that has advanced to clinical trials.

AN12855 (AN-12855) is potent, cofactor-independent M. tuberculosis InhA inhibitor, binds to and inhibits InhA with IC50 of 0.03 uM, shows potent activity against whole-cell M. tuberculosis H37Rv with IC90 of 0.09 uM; AN12855 demonstrates potent activity against drug-susceptible and drug-resistant strains of M. tuberculosis, exhibits comparable efficacy to the frontline antitubercular drug isoniazid (INH) in both acute and chronic models of TB infection with a lower potential for resistance development and shows in vitro activity against conventional KatG-mediated INH-resistant M. tuberculosis.

Antimicrobial peptide BING (IRIILRAQGALKI) is a thermostable 13-residue peptide that targets bacterial envelope stress response by suppressing cpxR expression in Gram-negative bacteria.BING downregulates efflux pump components and synergises the effect of antibiotics, and suppresses the development of antibiotic resistance.BING downregulated the expression of efflux pump components mexB, mexY and oprM in P. aeruginosa and significantly synergised the toxicity of antibiotics towards these bacteria.

ARN-75039 (ARN75039) is a potent, small molecule fusion inhibitor of arenavirus, inhibits pseudotyped entry of pGTOV and pCHAPV with EC50 of 0.13 and 4.3 nM, respectively.ARN-75039 demonstrated sub-nanomolar EC50 activity against pTCRV that further translated to native wild-and NWAs, including LASV, JUNV and MACV, in pseudotyped virus assays and against native replicative LASV and JUNV.ARN-75039 also potently inhibits mutant T434I pTCRV variant with EC50 of 29 nM.ARN-75039 dramatically improved survival outcome and potently inhibited TCRV replication in serum and various tissues at doses of 10 and 35 mg/kg, provided highly significant post-exposure protection in mice against TCRV infection.

ARN-75041 (ARN75041) is a potent, small molecule fusion inhibitor of arenavirus, inhibits pseudotyped entry of pGTOV and pCHAPV with EC50 of 1.7 and 15.3 nM, respectively. ARN-75041 demonstrated sub-nanomolar against native replicative LASV (LASV EC90<0.3 nM) and JUNV (EC90=6.2 nM).ARN-75041 also potently inhibits mutant T434I pTCRV variant with EC50 of 29 nM.ARN-75041 dramatically improved survival outcome and potently inhibited TCRV replication in serum and various tissues at doses of 10 and 35 mg/kg, provided highly significant post-exposure protection in mice against TCRV infection.

Azoffluxin (CMLD012336) is a bis-benzodioxolylindolinone that synergizes with fluconazole against C. auris through the inhibition of efflux pump Cdr1, thus increasing intracellular fluconazole levels.Azoffluxin increases intracellular accumulation of fluconazole (FLC) by inhibiting Cdr1-mediated efflux in C. auris.Azoffluxin potentiates intracellular acting compounds against C. auris, to a similar degree as deletion of CDR1.Azoffluxin is active against diverse C. auris strains, azoffluxin potentiated fluconazole in multiple isolates from three of the four major clades. The clade III isolates from South Africa were the exception.Azoffluxin enhances fluconazole (FLC) activity against azole-resistant C. albicans isolates.Azoffluxin not only enhanced fluconazole activity but also reduced fungal burden by ~1000-fold as a single agent in mice infected with drug-resistant C. auris.

BDM88855 Hcl is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BDM88855 is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BLI-489 is a bicyclic penem inhibitor that inhibits class A, C, and D beta-lactamases with synergistic effects with piperacillin; The combination of piperacillin-BLI-489 demonstrated improved activity compared to that of piperacillin-tazobactam against the problematic extended-spectrum beta-lactamase- and AmpC-expressing strains.

Burkfloxacin (BFX) is a fluoroquinolone analog that potently inhibits growth of intracellular Burkholderia.Burkfloxacin is active against other gram-negative organisms in vitro, showing similar potency to the widely used fluoroquinolone, ciprofloxacin (Cip), against Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853.Burkfloxacin near-completely inhibits plaque formation by Bt and Bp at concentration of 0.5 uM.Burkfloxacin functions as a canonical fluoroquinolone by inhibiting the negative DNA supercoiling activity of E. coli DNA gyrase.Treatment with Burkfloxacin was significantly more effective than ceftazidime, the current antibiotic of choice, for improving survival and decreasing bacterial counts in major organs in a murine model of fulminant respiratory melioidosis.

CBR417 (CBR-417) is a potent and selective antiwolbachial activity compound (Anti-Wolbachia wMel In vitro HCI cell-based assay IC50=21 nM, IC90=1640 nM).CBR417 demonstrates potent antiwolbachial activity was confirmed in L. sigmodontis, Brugia malayi, and Onchocerca ochengi in vivo preclinical models of filarial disease.CBR417 demonstrates in vitro selectivity against Loa loa (a safety concern in endemic areas).

CBS1194 is a novel specific fusion inhibitor for group 2 influenza viruses, inhibits IAVs bearing group 2 HAs (pseudo-H7, EC50=0.25 uM).CBS1194 displays no inhibition against both pseudo-H5 and pseudo-Lassa.CBS1194 exhibitss potency agianst group II influenza viruses influenza A/rhea/North Carolina/1993 (H7N1) and A/Hong Kong/1/1968 (H3N2) with EC59 of 3.17 and 1.60 uM, respectively.CBS1194 displays no inhibitory activity against group 1 influenza viruses, including A/Puerto Rico/8/1934 (H1N1) and A/Viet Nam/1203/04 (H5N1).CBS1194 acts at an early stage of viral infection, inhibits viral HA mediated hemolysis, and prevents the low pH-induced conformational change of HA.The substitutions K1172N and T301A but not D71N to confer resistance to CBS1194.

Ciapavir (SBI-0953294, cIAP1 antagonist for viral reactivation) is a bivalent, next-generation, Smac mimetic and antagonist of cIAP1 as latency-reversing agent (LRA), specifically and potently promote HIV-1 latency reversal activity both in vivo.Ciapavir's latency reversal activity is dependent on the NIK-dependent NF-κB signaling.Ciapavir exhibits substantially greater potency and efficacy as an LRA, inducing comparable levels of latency reversal at concentrations 10- to 1,000-fold lower than the first-generation molecule SBI-0637142, without an increase in cytotoxicity.Ciapavir does not trigger cytokine release or T cell activation.Ciapavir is capable of increasing latent HIV-1 expression in ART-treated BLT mice in vivo and may therefore prove useful in "shock and kill" approaches to HIV-1 cure.

COR388 (Atuzaginstat) is an orally bioavailable, brain penetrant small-molecule that irreversibly inhibits lysine-gingipain (Kgp, gingipain K) with Ki of <0.01 nM.COR388 blocks the activity of gingipains, a type of toxic protein made by the bacteria Porphyromonas gingivalis ( P. gingivalis ).COR388 reduced the bacterial load of an established P. gingivalis brain infection, blocked Aβ1-42 production, reduced neuroinflammation, and rescued neurons in the hippocampus.

COR588 is a second-generation small-molecule lysine-gingipain (Kgp, gingipain K) inhibitor with novel structure and improved pharmacologic and safety profile prioritized for Alzheimer’s development.

CTCB-405 (CTCB405) is a small molecule allosteric inhibitor of T. brucei phosphofructokinase (TbPFK) with IC50 of 0.18 uM, ITC Kd of 92 nM, no significant inhibition of human PFKs.CTCB-405 demonstrated in vitro parasite killing potency of the bloodstream form of T. brucei strain Lister 427 (EC50=0.37 uM).CTCB-405 (50, 100 mg/kg) clear parasites in a stage 1 model of HAT infection with 1-day oral dosing and show reduction of parasitaemia in the brain in a pleiomorphic model.

CTN1122 (CTN-1122) is a potent, selective Leishmaniacasein kinase 1 isoform 2 (CK1.2, L-CK1.2) with IC50 of 0.72 uM (LmCK1) and 0.8 uM (amastigotes L. major), antileishmanial compound.

Dichlorcyclizine (DCCZ) is a potent, small molecule HCV fusion inhibitor, also inhibits SARS-CoV and SARS-CoV-2 S-mediated infection in MA104 cells with EC50 of 9.92 and 4.53 uM, respectively.

DMA-135 (DMA135) is a RNA-biased small molecule binds to the EV71 SLII IRES domain (Kd=520 nM), dose-dependently (IC50=7.54 uM) inhibits EV-71 viral translation and replication.DMA-135 inhibits EV71 replication by attenuating IRES-dependent translation at dosages of relatively low cellular toxicity.DMA-135 changes the local and global structure of the EV71 SLII IRES domain.DMA-135 allosterically stabilizes a AUF1 (cellular protein)-SLII-(DMA-135) ternary complex.

DMA-135 (DMA135) is a RNA-biased small molecule binds to the EV71 SLII IRES domain (Kd=520 nM), dose-dependently (IC50=7.54 uM) inhibits EV-71 viral translation and replication.DMA-135 inhibits EV71 replication by attenuating IRES-dependent translation at dosages of relatively low cellular toxicity.DMA-135 changes the local and global structure of the EV71 SLII IRES domain.DMA-135 allosterically stabilizes a AUF1 (cellular protein)-SLII-(DMA-135) ternary complex.

DNA gyrase inhibitor EN-7 (EN-7) is a potent bacterial DNA gyrase inhibitor, is active against pathogenic species that are resistant to ciprofloxacin and other clinically important antibiotics.EN-7 inhibited growth of the wild-type strain (S. aureus) with MIC 1 μM.Strains containing GyrA A34T (mut-3 and mut-9), GyrA P219Q (mut-6), and GyrB K417E (mut-1, mut-2, mut-4, and mut-5) exhibited moderate resistance, with MICs of either 4 or 8 μM.EN-7 inhibited sporulation pathway in the bacterial genus Streptomyces.

DU011 is a noncanonical anti-infective agent and small-molecule inhibitor of capsule biogenesis, targets MprA (Kd=30 nM), a MarR family transcriptional repressor of multidrug efflux pumps, inhibits capsule expression in E. coli. DU011 does not alter Escherichia coli antibiotic resistance and has significantly enhanced inhibition of capsule expression, compared with other proposed MprA ligands, such as salicylate and 2,4-dinitrophenol (DNP).

Durlobactam is a novel beta-lactamase inhibitor for treatment of resistant bacterial infections.

EC-11716 (EC/11716) is a novel mycobacterium tuberculosis gyrase inhibitor with potent anti-tubercular activity (MIC 0.38 uM, M. tuberculosis H37Rv).EC/11716 is active against M. abscessus subspecies and clinical isolates, maintains comparable activity against a panel of clinical isolates covering the M. abscessus complex.EC/11716 is effective against M. abscessus biofilms (MIC 0.78 uM), with better bactericidal activity against biofilms than moxifloxacin.EC/11716 is active against M. abscessus in vivo.

Elunonavir is an azapeptide atazanavir analogs useful for treating HIV infections.

FC-8052 (FC8052) is a highly potent inhibitor of HIV-1 Nef-effector kinase, binds to recombinant Nef in vitro with Kd of 10 pM; FC-8052 inhibits Nef-dependent HIV-1 replication in PBMCs in the subnanomolar range.

FD028 is a small-molecule HIV-1 inactivator by conjugating FD016 (gp120-CD4 binding inhibitor) with FD017 (HIV-1 fusion inhibitor), inactivates cell-free virions (IC50=0.7 uM) of by targeting both HIV-1 gp120 and gp41.FD028 is not significantly toxic and has broad-spectrum HIV-1 inhibitory and inactivation activity, including T20-resistant viruses and T2635-resistant viruses.

FG944 (FG-944) is a potent selective LpxC inhibitor with MIC50 of 0.5 ug/mL against K.pneumoniae, synergizes with rifampin in carbapenem resistant K. pneumoniae and E. coli.

Filovirus inhibitor compd-A is a small molecule filovirus entry inhibitor targeting the endosomal receptor NPC1 binding site, shows potent inhibitory activity against both Ebola and Marburg viruses with IC50 of 0.86 uM against pseudotyped Marburg virus entry.

FIM1033 (FIM-1033) is a potent small-molecule inhibitor of FimH with HAI EC90 of 8 nM, with antibiotica activities, significantly attenuated bacterial loads in pyelonephritis in treated mice.

Fluoxazolevir (NCGC00351982) is a potent, small molecule entry inhibitor of HCV with EC50 of 18.8 nM.Fluoxazolevir inhibits fusion of HCV with hepatic cells by binding HCV envelope protein 1 (E1) to prevent fusion.Fluoxazolevir was generally effective against all chimeric HCV-RLuc genotypes including 1a, 1b, 2b, 3a, 4a, 5a, 6a and 7a, was most effective against HCV 2a and 2b, followed by 3a and 6a, all within sub-μM EC50 values, with little to no cytotoxicity (CC50>20 uM).Fluoxazolevir was highly synergistic with other anti-HCV drugs (interferon-α, ribavirin, daclatasvir, sofosbuvir and simeprevir (NS3/4A protease inhibitor)).Fluoxazolevir suppresses HCV infection in humanized chimeric mice, and is active against multidrug-resistant HCV.Fluoxazolevir also broadly blocked human coronavirus entry into various cell types, inhibit SARS-CoV S- and SARS-CoV-2 S-mediated infection MA104 cells with EC50 of 6.49 and 3.86 uM, respectively.

GaMF1 is a novel antimycobacterial compound that targets the F1FO-ATP synthase γ subunit loop; GaMF1 is bactericidal and is active against multidrug- as well as bedaquiline-resistant strains. Combining GaMF1 with bedaquiline or novel diarylquinoline analogues showed potentiation without inducing genotoxicity or phenotypic changes in a human embryonic stem cell reporter assay. GaMF1 presents an attractive lead for the discovery of a novel class of anti-tuberculosis F-ATP synthase inhibitors.

GC-072 (GC072) is a potent, 4-oxoquinolizine antibiotic with selective inhibitory activity against bacterial topoisomerases (E. coli Topo II/DNA gyrase, IC50=0.18-1.5 uM).GC-072 demonstrated no detectable inhibition of human Topo I and II, is selective for bacterial topoisomerases (IC50>100 uM).GC-072 inhibits E. coli Quinolone-resistant gyrase (IC50=1.3-1.5 uM), S. aureus Gyrase and Topo IV (IC50=2-30 uM).GC-072 demonstrated good activity against B. pseudomallei, with an MIC90 of 0.25 ug/mL.GC-072 exhibited strong in vitro antimicrobial potency against biothreat agents Bacillus anthracis, Yersinia pestis, and Francisella tularensis and category B biothreat agent Burkholderia mallei.GC-072 is efficacious against B. pseudomallei aerosol infection in a mouse model following exposure to a 24-LD50 bacterial challenge.

GHP-88309 (GHP88309) is a non-nucleoside, broad-spectrum allosteric inhibitor of paramyxovirus polymerase with EC50 of 0.9 uM against HPIV3-JS RdRP.Demonstrates highly potent antiviral potency against HPIV3-JS and clinical isolates HPIV3-9R4 and HPIV3-10L3 in the primary cell/virus isolate system (EC50=0.07-0.08 uM), without cytotoxicity.GHP-88309 targets a conserved microdomain in the L protein, inhibiting de novo RNA synthesis.GHP-88309 is efficacious in well-differentiated human airway epithelium cultures grown at air-liquid interface (3D-ALI-HBTEC).GHP-88309 (150 mg/kg b.i.d.) is orally efficacious in HPIV disease surrogate model.GHP-88309 possesses unusual broad-spectrum activity against diverse paramyxoviruses including respiroviruses (i.e. HPIV1 and HPIV3) and morbilliviruses (i.e. MeV).

GRL-079 is a novel potent, nonpeptidic HIV-1 protease inhibitor with 2.5-30 nM against wild-type HIV-1NL4-3, 0.3-6.7 nM against HIV-2EHO, and 0.9-90 nM against laboratory-selected-PI-resistant HIV-1 and clinical HIV-1 variants resistant to multiple FDA-approved PIs (HIVMDR).

GSK-229423 is a novel bacterial topoisomerase inhibitor that shows potent inhibition of supercoiling by DNA gyrase from S. aureus with IC50 of 14 nM; displays approximately 70 times more potent against S. aureus DNA gyrase than NXL101; has potent antibacterial activity against a broad spectrum of Gram-positive and Gram-negative bacterial pathogens, including clinical isolates with fluoroquinolone resistance mediated by DNA gyrase and topo IV mutations.

GSK-2336805 (JNJ-56914845) is a novel potent HCV NS5A inhibitor with multigenotype activity, has EC50s of 58.5, 7.4, and 53.8 pM on genotype 1a (H77), genotype 1b (Con-1 ET), and genotype 2a (JFH-1) replicon cells; shows an average EC50 of 63.7 pM on genotype 2a Jc1 virus, inhibits the HCV replication cycle and production of virus; retains activity on chimeric replicons containing NS5A patient sequences from genotype 1 and patient and consensus sequences for genotypes 4 and 5 and part of genotype 6.

GSK 3011724A (DG-167, GSK-3011724A) is a potent, specific inhibitor of β-ketoacyl-ACP synthase (KasA, Kd=9 nM), shows anti-tubercular activity (MIC H37Rv=0.8 uM); shows much weaker apparent dissociation constant for both Pks10 and Pks (Kd=1.4 uM); inhibits mycolic acid biosynthesis and shows negligible activity against a panel of unrelated proteins and 18 Gram-positive and Gram-negative bacterial species.

GSK3739936 (BMS-986180) is a potent, allosteric HIV-1 integrase (ALLINI), shows excellent potency in vitro against majority of the 124/125 variants (EC50=1.7 nM).

GSK693 (GSK-693) is a potent, direct inhibitor of M. tuberculosis enoyl-ACP reductase (InhA) with IC50 of 7 nM, shows equally potent activity against M. tuberculosis H37Rv both intra and extracellularly (MIC=0.2 uM); exhibits activities against multidrug (MDR) and extensively (XDR) drug-resistant clinical isolates as well as in TB murine models when orally dosed.

GW461484A (GW-461484A) is a potent small molecule capable of restoring caspofungin sensitivity, inhibits Yck2 kinase in C. albicans, originally discovered as an inhibitor of human p38α with IC50 of 150 nM.GW461484A inhibited a very narrow spectrum of human kinases. At 1 uM, it showed >80% binding to only 10 additional human kinases out of a panel of >400 kinases.Yck2 is the proximal target of GW responsible for restoration of echinocandin sensitivity in C. albicans, potently inhibits Yck2 kinase activity in vitro and impairs the virulence of C. albicans in co-cultures and in mice.GW461484A potentiates conventional antifungals against a broad range of pathogens.

HHV protease inhibitor 43 is an irreversible small molecule inhibitor of human herpesvirus (HHV) protease targeting a non-catalytic cysteine (C161) with IC50 of 4 uM (HCMV), exhibits broad-spectrum inhibition of other HHV protease homologs.HHV protease inhibitor 43 demonstrates inhibitor stabilization of HCMV Pr homodimerization, exploiting a conformational equilibrium to block proteolysis.HHV protease inhibitor 43 causes a dose-dependent decrease in HCMV replication in HFF-1 cells with IC50 of 5 uM, with no significant cytotoxicity (CC50>20 uM).

HIV-1 inhibitor 5b is a novel anti-HIV-1 compound that inhibits HIV-1 JR-CSF with EC50 of 1 nM without significant cytotoxicity (CC50>20 uM), also shows potency against NRTI- and NNRTI-resistant HIV-1 (EC50=1-3 nM); shows a chemical backbone similar to the clinically used integrase (IN) strand transfer inhibitor (INSTI) elvitegravir, but has no detectable INSTI activity; various drug-resistant HIV-1 strains did not display cross resistance to HIV-1 inhibitor 5b; remains its anti-HIV-1 activity even after the viral integration stage, significantly suppresses p24 antigen production in HIV-1 latently infected cells exposed with TNF-alpha; demonstrates favorable pharmacokinetic profiles in mice.

HIV-1 Integrase inhibitor GS-B (GS-B) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 8.1 nM.GS-B displays antiviral potency in MT-4, MT-2, and human PBMCs with EC50 values of 18, 10, and 21 nM, respectively.

IM-250 is a potent HSV-1 helicase primase inhibitor, inhibits HSV-1 replication with IC50 of 20 nM (clinical isolate of HSV-1).IM-250 dispalys similar IC50 values (20-30 nM) against ACV-resistant HSV-1 clinical isolates 2 and 3 and ACV-resistant HSV-2 clinical isolates 7 and 8.IM-250 exhibits a broad therapeutic window against HSV-1 in vitro with pronounced higher SI values as obtained for acyclovir (ACV).IM-250 shows in vivo efficacy and attenuates viral burden in HSV-1 infection mouse model.

IY7640 (IY-7640) is a small molecule targeting the stalk region of the influenza HA protein, blocks HA-mediated membrane fusion of H1N1, H3N2, and influenza B viruses in cells.IY7640 demonstrated potency against H1N1, H3N2, H5N1, H7N9, and H9N2 subtypes of IAV, including the 2009 pandemic H1N1 (pH1N1) virus (A/Korea/01/2009, rK09), with EC50 of 0.62-220 uM in plaque reduction assay in MDCK cells.IY7640 successfully inhibited rK09 replication in cells at a level comparable to that of oseltamivir, K09 HA fusion was inhibited only by 1 uM IY7640.The stalk region of the influenza HA protein is highly conserved across different (sub)types of influenza viruses.

JCP276 is a novel antibiotic and covalent inhibitor that disrupt M. tuberculosis growth by targeting multiple serine hydrolases.JCP276 is a narrow-spectrum inhibitor of Mycobacterium tuberculosis growth.JCP276 inhibits multiple nonessential serine hydrolases.JCP276 treatment caused accumulation of free lipids and a substantial decrease in lipooligosaccharides, linking SH inhibition to defects in cell envelope biogenesis.

JMN3-003 is a host-directed inhibitor with potent antiviral activity against a panel of myxovirus family members with EC50 of 10-70 nM.JMN3-003 shows activity against MeV at 170 (viral CPE-reduction assay) and 30 nM (virus yield reduction assay) and does not display any detectable acute cytotoxicity.JMN3-003 also shows superb antiviral activity against a selection of clinical-relevant paramyxovirus (RSV, MuV, and HPIV3) and orthomyxovirus (influenza) family members.

JTP-0157602 (JTP0157602) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 4.2 nM.JTP-0157602 exhibits potent antiviral activity against HIV-1 with EC90 of 138 nM.JTP-0157602 retained potent antiviral activity (EC50=1-6 nM) against a broad panel of recombinant viruses with INSTI-related resistant mutations, including multiple substitutions that emerged in clinical studies of INSTIs (IN strand transfer inhibitors (INSTIs).JTP-0157602 inhibited HIV-1 replication mainly during the late-phase of the replication cycle.JTP-0157602 binds to the LEDGF/p75 binding pocket of HIV-1 integrase (IN).

KNI-1657 (KNI1657) is a highly potent HIV-1 protease inhibitor (97% inhibition at 1 nM) with high sensitivity against lopinavir/ritonavir- or darunavir-resistant strains; inhibits wild-type HIV-1 (pNL4-3) and LPV-resistant strain A17 with IC50 of <3 and 25 nM, respectively.

KYT-1 is a potent, selective inhibitor of P. gingivalis virulence factor Arg-gingipain (Rgp) with Ki 40 nM (RgpA/B).KYT-1 showed significant inhibitory effects on SMC proliferation stimulated by Porphyromonas gingivalis.

KYT-36 is a potent, selective, and bioavailable inhibitor of P. gingivalis virulence factor gingipain K (Kgp, lysine-gingipain), potently and selectively inhibits Kgp with Ki of 0.27 nM, respectively.KYT-36 consists of benzyloxycarbonyl (BOC), L-glutaminyl (GLN), methylphenylamino (MPA), L-lysinyl (LYS), and benzylcarbamoyl (BCA) moieties.KYT-36 strongly inhibited degradation of host proteins in culture supernatants and abolished thriving of P. gingivalis in cell cultures and in periodontal pockets in vivo.KYT-36 prevented Kgp-triggered vascular permeability in guinea pigs, i.e. demonstrating its efficacy against bacterial virulence in vivo, with no toxicity effects.

LFF571 is a semisynthetic thiopeptide and bactericidal antibiotic that interferes with bacterial protein synthesis by inhibition of elongation factor EF-Tu, LFF571 is potent in vitro activity against C.difficile strains with MIC90 of 0.25 ug/mL.LFF571 demonstrated activity against most other Gram-positive rods and cocci (MIC50/90, 0.125/0.25 μg/mL) except for bifidobacteria and some species of lactobacilli, showed reduced active activity against Gram-negative anaerobes with MICs for Bacteroides fragilis of 4 and 8 μg/mL.LFF571 inhibits exogenous protein synthesis elongation factor EF-Tu and interferes with the ability for EF-Tu to deliver aminoacylated tRNA to the ribosome.

LPXC-516 is a potent bacterial LpxC inhibitor with IC50 of 0.68 nM (P. aeruginosa LpxC), potent against the P. aeruginosa isolates with MIC90 of 2 ug/mL.

MBX3132 is a small mocule inhibitor of AcrB multidrug efflux pump, fully potentiates the activity of a broad range of antibiotics at 0.1 uM; does not exhibit membrane-disrupting or antibacterial activity.

MCB 3681 is a quinolonyl-oxazolidinone bactericidal antibiotic, has activity in vitro against Gram-positive bacteria. MCB3681 has a potent in vitro activity against C. difficile with MIC90 of 0.064 ug/ml.

mCLB073 (mCLB 073) is a more potent, specific, oral small molecule agonist of the Mtb adenylyl cyclase Rv1625c, an optimized analog of the V-59 for in vivo use.mCLB073 exhibited 17-fold potency improvement against Mtb in cholesterol media relative to V-59 while maintaining excellent pharmacokinetic properties and a good safety profile.mCLB073 (30 mg/kg, oral) reduced Mtb CFUs in the lungs of mice significantly and decreased the extent of lung pathology by 45%.

MGB-BP-3 is a potent bactericidal antibiotic with a completely novel mode of action, selectively binds to the minor grove of microbial DNA, has the potential for Clostridioides difficile infection (CDI).

MMV019721 (MMV019721) is an antiplasmodial drug-like compound tageting Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS), directly and selectively inhibit PfAcAS activity in vitro with IC50 of 73 nM.MMV019721 directly inhibits PfAcAS by preventing CoA binding.MMV019721 has activity against blood-stage parasites in vitro (P. falciparum 3D7, EC50=460 nM) and against liver-stage P. berghei parasites (Pbluc EC50=2,000 nM).MMV019721 directly and selectively inhibits PfAcAS activity in vitro.

MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation, shows potent activity against liver, asexual, and sexual blood stage development.MMV030084 showed an IC50 of 109 nM against the drug-sensitive 3D7-A10 line, and an IC50 of 120 nM against multidrug-resistant Dd2-B2 parasites in a 72-h growth inhibition assay against Pf ABS parasites.MMV030084 inhibited male gamete exflagellation at an IC50 of 141 nM when gametocytes were stimulated to develop into male gametes.MMV030084 is a promising Plasmodium PKG-targeting chemotype.

MMV084978 (MMV 084978) is an antiplasmodial drug-like compound tageting Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS), directly and selectively inhibit PfAcAS activity in vitro with IC50 of 370 nM.MMV084978 directly inhibits PfAcAS by preventing CoA and acetate binding.MMV084978 demonstrated in vitro efficacy (P. falciparum Dd2 EC50=150 nM) with increased liver-stage potency (Pbluc EC50= 520 nM).MMV084978 directly and selectively inhibit PfAcAS activity in vitro.

MMV675968 is a potent, small molecule inhibitor of Toxoplasma gondii (T. gondii) with IC50 of 0.02 uM, via the pathogen box.MMV675968 has been shown to be efficient against the planktonic form of C. albicans.MMV675968 showed an antiplasmodial activity against P. falciparum.MMV675968inhibited the growth of all four A. baumannii test strains with IC50 of 0.6-2.7 uM, IC90 of 0.7-3.9 uM, and MIC of 1.6-10 uM.

MMV688533 is a potent antimalarial compound that displays fast parasite clearance in vitro and is not cross-resistant with known antimalarials, MMV688533 is highly potent against multiple P. falciparum strains with IC50 values in low nanomolar range (P. falciparum 3D7, IC50=1.9 nM).MMV688533 also showed excellent ex vivo activity against asexual blood-stage parasites from fresh P. falciparum isolates (median IC50=1.3 nM, range=0.02 to 6.3 nM).MMV688533 remained potent in ex vivo assays against both P. falciparum and P. vivax with IC50 of 18.9 and 12.0 nM respectively.MMV688533 displayed fast and potent in vivo efficacy and favorable in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetic properties.MMV688533 antiplasmodial activity is unrelated to existing antimalarials and selects for low-grade resistance mediated in part by mutations in PfACG1 and PfEHD.

MMV688844 (MMV844) is a piperidine-4-carboxamide with bactericidal properties against M. abscessus, targets mycobacterial DNA gyrase.

Mtb CoaBC inhibitor 1f is a direct small molecule inhibitor of Mtb 4'-phosphopantothenoyl-l-cysteine synthetase (PPCS, CoaB) domain of the bifunctional Mtb CoaBC (IC50=15.6 uM).Mtb CoaBC inhibitor 1f inhibit CoaBC uncompetitively with respect to 4'-phosphopantothenate, the substrate for the CoaB-catalyzed reaction.Mtb CoaBC inhibitor 1f inhibits Mtb growth in whole-cell activity against Mtb H37Rv (MIC=25.9 uM).

N205 is a novel anti-malaria compound with in vitro IC50 of 1.3 nM against Plasmodium falciparum (3D7); demonstrates excellent rodent pharmacokinetic and in vivo antimalarial efficacy studies in the mouse Plasmodium berghei and Plasmodium falciparum Pf3D70087/N9 severe combined immunodeficiency (SCID) mouse models.

NBD-14273 is a CD4-mimetic, small-molecule HIV-1 entry inhibitor with IC50 of 0.13 uM.NBD-14273 showed both improved antiviral activity and selectivity index (SI) against HIV-1HXB2 compared to NBD-14136.NBD-14273 displayed potenct against a large panel of 50 HIV-1 Env-pseudotyped viruses representing clinical isolates of diverse subtypes.

NEU-4438 (NEU4438) is a potent inhibitor of P. falciparum with EC50 of 13 nM (T. brucei), demonstrates improved aqueous solubility (880 uM) compared to NEU-1953; reduced parasitemia 109 fold in trypanosome-infected mice.

NPG9 (NSR inhibitor NPG9) is a small molecule inhibitor of streptococcus agalactiaenisin resistance protein (NSR) with 58% inhibition at 100 uM (specific growth inhibition assay).

PDE-I2 is a potent and selective inhibitor of malaria proliferation with Pf IC50 of 18 nM.PDE-I2 is a precursor of the anticancer duocarmycin family that preserves the class's sequence-specific DNA binding but lacks its signature DNA alkylating cyclopropyl warhead.PDE-I2 retains comparable antimalarial potency to chloroquine.PDE-I2 is >1,000-fold less toxic to human cell lines than duocarmycin, with mitigated impacts on eukaryotic chromosome stability.PDE-I2 treatment induces severe defects in parasite nuclear segregation leading to impaired daughter cell formation during schizogony.

PTC-672 (PTC672) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.4 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-672 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-672 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-672 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-672 showed 78% inhibition at 2.5 μM aginst Ng RNR activity, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.PTC-672 (30 mg/kg) demosntrates in vivo efficacy in a mouse model of gonorrhea.

PTC-847 (PTC847) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.1 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-847 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-847 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-847 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-847 showed 93% inhibition aginst Ng RNR activity at 4 uM, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.

Q308 is a small molecule that silences the latent HIV-1 provirus by inhibiting Tat-mediated gene transcription and selectively downregulates the expression levels of the facilitated chromatin transcription (FACT) complex.Q308 induced the preferential apoptosis in HIV-1 latently infected cells, Q308 may reduce the size of the viral reservoir.

Quabodepistat (OPC-167832) is a highly potent antituberculosis agent with MIC of 0.00024 to 0.002 ug/mL against Mycobacterium tuberculosis, targets DprE1 (IC50=258 nM, recombinant DprE1), an essential enzyme for cell wall biosynthesis.OPC-167832 showed MIC90 of 0.0048 and 0.0027 ug/mL against intracellular M. tuberculosis strains H37Rv and Kurono were 0.0048 and 0.0027, respectively.OPC-167832 showed potent bactericidal activities starting at a dose of 0.625 mg/kg of body weight in a mouse model of chronic TB.OPC-167832 exhibited significant combination effects in 2-drug combinations with delamanid, bedaquiline, or levofloxacin.

QZN 34 is a small molecule pseudomonas aeruginosa PQS quorum-sensing system (PqsR) inhibitor with IC50 of 15 uM, kills planktonic Gram-positives (S. aureus, MIC 6.25 uM) but not Gram-negatives.QZN 34 prevented S. aureus biofilm formation, severely damaged established S. aureus biofilms, and perturbed P. aeruginosa biofilm development.QZN 34 killed planktonic Gram-positive pathogens including S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, and Clostridioides difficile but not Gram-negative bacteria such as P. aeruginosa and Escherichia. coli.QZN 34 eradicated the mixed-species biofilm against mixed S. aureus and P. aeruginosa biofilms when combined with aminoglycoside.