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.

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.

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.

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.

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.

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.

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).

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.

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.

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.

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.

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.

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).

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.

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.

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).

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-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.

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).

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).

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.

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.

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.

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.

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.

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.

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.

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.

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.

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