| DC70326 |
CTCB-405 |
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. |
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| DC70328 |
CTN1122 |
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. |
|
| DC70356 |
Dichlorcyclizine |
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. |
|
| DC70361 |
DMA-135 freebase |
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. |
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| DC70362 |
DMA-135 |
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. |
|
| DC70364 |
DNA gyrase inhibitor EN-7 |
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. |
|
| DC70368 |
DU011
Featured
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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). |
|
| DC70370 |
Durlobactam |
Durlobactam is a novel beta-lactamase inhibitor for treatment of resistant bacterial infections. |
|
| DC70376 |
EC-11716 |
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. |
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| DC70382 |
Elunonavir
Featured
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Elunonavir is an azapeptide atazanavir analogs useful for treating HIV infections. |
|
| DC70402 |
FC-8052 |
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. |
|
| DC70403 |
FD028 |
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. |
|
| DC70407 |
FG-944 |
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. |
|
| DC70410 |
Filovirus inhibitor compd-A |
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. |
|
| DC70411 |
FIM1033 |
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. |
|
| DC70414 |
Fluoxazolevir |
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. |
|
| DC70424 |
GaMF1 |
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. |
|
| DC70428 |
GC-072 |
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. |
|
| DC70432 |
GHP-88309 |
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). |
|
| DC70443 |
GRL-079 |
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). |
|
| DC70455 |
GSK-229423 |
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. |
|
| DC70456 |
GSK-2336805 |
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. |
|
| DC70459 |
GSK3011724A
Featured
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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. |
|
| DC70464 |
GSK3739936 |
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). |
|
| DC70470 |
GSK693 |
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. |
|
| DC70474 |
GW461484A |
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. |
|
| DC70484 |
HHV protease inhibitor 43 |
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). |
|
| DC70486 |
HIV-1 inhibitor 5b |
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. |
|
| DC70487 |
HIV-1 Integrase inhibitor GS-B |
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. |
|
| DC70505 |
IM-250
Featured
|
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. |
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