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Browse result page of AntiTbPdb

The total number entries retrieved from this search are 48
IDNameSequenceN-Terminal ModificationC-Terminal ModificationChemical ModificationLinear/CyclicLengthChiralityNatureSourceOriginSpeciesStrainInhibition ConcentrationIn vitro/ In vivoCell LineIntracellular InhibitionCytotoxicityAnimal ModelEffective Dose in model organismImmune ResponceMechanism of ActionTargetCombination TherapyOther ActivitiesYear of PublicationPubmed ID/ Patent No.
antitb_1195Boropentapeptide AVKAA-B(OH)2 FreeConjugated with Boronic acidConjugated with Boronic acidLinear5LNASyntheticNAMycobacterium thermoresistible Mycobacterium thermoresistible Poorer inhibition than Pinanediol PD-protected Boropentapeptide In vitroNoneNANANone NANAInhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB))Mycosin protease-1 (MycP1) NoneNone201424915878
antitb_1196Boropentapeptide AVKAA-B(OH)2 FreeConjugated with Boronic acidConjugated with Boronic acidLinear5LNASyntheticNAMycobacterium smegmatis Mycobacterium smegmatis Poorer inhibition than Pinanediol PD-protected Boropentapeptide In vitroNoneNANANone NANAInhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB))Mycosin protease-1 (MycP1) NoneNone201424915878
antitb_1197Boropentapeptide AVKAA-B(OH)2 FreeConjugated with Boronic acidConjugated with Boronic acidLinear5LNASyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis Poorer inhibition than Pinanediol PD-protected Boropentapeptide In vitroNoneNANANone NANAInhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB))Mycosin protease-1 (MycP1) NoneNone201424915878
antitb_1198Pinanediol PD-protected Boropentapeptide AVKAA-BO2(PD) FreeConjugated with Boronic acid and pinanediol PDConjugated with Boronic acid and pinanediol PDLinear5LNASyntheticNAMycobacterium thermoresistible Mycobacterium thermoresistible IC50 = 121.6 ± 25.3 μM for MycP1In vitroNoneNANANone NANAInhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB))Mycosin protease-1 (MycP1) NoneNone201424915878
antitb_1199Pinanediol PD-protected Boropentapeptide AVKAA-BO2(PD) FreeConjugated with Boronic acid and pinanediol PDConjugated with Boronic acid and pinanediol PDLinear5LNASyntheticNAMycobacterium smegmatis Mycobacterium smegmatis IC50 = 93.2±33.7 μM for MycP2In vitroNoneNANANone NANAInhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB))Mycosin protease-1 (MycP1) NoneNone201424915878
antitb_1200Pinanediol PD-protected Boropentapeptide AVKAA-BO2(PD) FreeConjugated with Boronic acid and pinanediol PDConjugated with Boronic acid and pinanediol PDLinear5LNASyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis IC50 = 37.9±5.2 μM for MycP3In vitroNoneNANANone NANAInhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB))Mycosin protease-1 (MycP1) NoneNone201424915878
antitb_1271Inhibitor 1PK-(boroMet)AcetylationFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1272Inhibitor 2HK-(boroMet)AcetylationFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1273Inhibitor 3AK-(boroMet)AcetylationFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1274Inhibitor 4Ala(1-naphtyl)-K-boroLeu FreeFreeAla(1-naphtyl) = 1-napthylalanine, boroLeu = leucine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1275Inhibitor 4Ala(1-naphtyl)-K-boroLeu FreeFreeAla(1-naphtyl) = 1-napthylalanine, boroLeu = leucine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium smegmatisMycobacterium smegmatis strain constitutively expressing GFP-ssrA MIC50 = 1.5 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1276Inhibitor 5WK-(boroMet) Addition of N-picolinoylFreeboroLeu = leucine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NASlight toxic (25%) at 10 μMNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1277Inhibitor 6AK-(boroMet) Addition of N-picolinoylFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1278Inhibitor 7PK-(boroMet) Addition of N-picolinoylFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 24 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1279Inhibitor 8K-(boroMet) Addition of N-picolinoylFreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1280Inhibitor 9K-(boroMet) Addition of N-(3-Phenyl)propanoyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1281Inhibitor 10K-(boroMet) Addition of N-(Benzyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1282Inhibitor 11K-(boroMet) Addition of N-(2-(3,5-Difluorophenyl)acetyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1283Inhibitor 12W-(boroMet) Addition of N-(2-(3,5-Difluorophenyl)acetyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1284Inhibitor 12W-(boroMet) Addition of N-(2-(3,5-Difluorophenyl)acetyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium smegmatisMycobacterium smegmatis strain constitutively expressing GFP-ssrA MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1285Inhibitor 13K-(boroMet) Addition of N-(1H-benzo(b)thiophene-7-carbonylFreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1286Inhibitor 14K-(boroMet) Addition of N-(Phenylmetanesulfonyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 200 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_13191-C134mer H-Ntridec-NLys-Nspe-Nspe-NLys-NH2FreeAmidationNlys = N-(4-aminobutyl)glycine, Nspe = (S)-N-(1-phenylethyl)glycine, Ntridec = N-(tridecyl)glycineLinear5LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37RvMIC = 6.6 μMIn vitroRaw 264.7 and J774 mouse macrophageNALD50 = >100 μMNA NANANANANANA201121464254
antitb_132014merH-NLys-Nspe-Nspe-NLys-NH2FreeAmidationNlys = N-(4-aminobutyl)glycine, Nspe = (S)-N-(1-phenylethyl)glycineLinear4LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37RvNAIn vitroRaw 264.7 and J774 mouse macrophageNANon toxicNA NANANANANANA201121464254
antitb_13251-C134mer H-Ntridec-NLys-Nspe-Nspe-NLys-NH2FreeAmidationNlys = N-(4-aminobutyl)glycine, Nspe = (S)-N-(1-phenylethyl)glycine, Ntridec = N-(tridecyl)glycineLinear5LCationicSyntheticNAMycobacterium bovis Mycobacterium bovis BCGMIC = 6.3 μMIn vitroRaw 264.7 and J774 mouse macrophageNALD50 = >100 μMNA NANANANANANA201121464254
antitb_132614merH-NLys-Nspe-Nspe-NLys-NH2FreeAmidationNlys = N-(4-aminobutyl)glycine, Nspe = (S)-N-(1-phenylethyl)glycineLinear4LCationicSyntheticNAMycobacterium bovis Mycobacterium bovis BCGMIC = >100 μMIn vitroRaw 264.7 and J774 mouse macrophageNANon toxicNA NANANANANANA201121464254
antitb_1371Mycobacterial tuberculosis DHFR tripeptide analogWYDFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 1.26 × 10−7in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1372Mycobacterial tuberculosis DHFR tripeptide analogWYEFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 5.02 × 10−6 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1373Mycobacterial tuberculosis DHFR tripeptide analogWPDFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 9.12 × 10−9 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1374Mycobacterial tuberculosis DHFR tripeptide analogWPEFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 1.02 × 10−6 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1375Mycobacterial tuberculosis DHFR tripeptide analogYPDFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 4.17 × 10−8 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1376Mycobacterial tuberculosis DHFR tripeptide analogYPEFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 2.75 × 10−8 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1377Mycobacterial tuberculosis DHFR tripeptide analogWYYFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 1.78 × 10−9 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1378Mycobacterial tuberculosis DHFR tripeptide analogWPYFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 9.55 × 10−8 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1379Mycobacterial tuberculosis DHFR tripeptide analogWYPFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 4.57 × 10−8 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1380Mycobacterial tuberculosis DHFR tripeptide analogWPWFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 4.27 × 10−6 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1381Mycobacterial tuberculosis DHFR tripeptide analogWYWFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 1.45 × 10−7 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1382Mycobacterial tuberculosis DHFR tripeptide analogWYSFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 1.44 × 10−8 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1383Mycobacterial tuberculosis DHFR tripeptide analogWPSFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 7.94 × 10−8 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1384Mycobacterial tuberculosis DHFR tripeptide analogWPTFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 2.95 × 10−7 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1385Mycobacterial tuberculosis DHFR tripeptide analogWYTFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 3.31 × 10−6 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1386Mycobacterial tuberculosis DHFR tripeptide analogYPSFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 8.91 × 10−6 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_1387Mycobacterial tuberculosis DHFR tripeptide analogYPTFreeFreeNoneLinear3LCationicSyntheticNAMycobacterium tuberculosisMycobacterium tuberculosisKd= 6.46 × 10−6 in silicoNANANANA NANANAmycobacteium tuberculosis DHFRNA200919697148
antitb_15561-C134merH-Ntridec-Nlys-Nspe-Nspe-Nlys_NH2FreeAmidationNlys = N-(4-aminobutyl)glycine, Nssb = (S)-N-(sec-butyl)glycineNA5LCationicNANAMycobacterium tuberculosisMycobacterium tuberculosis H37RvMIC = 6.3 μg/mlNANANANANA NANANANANANA201525613372
antitb_1607TP-5RKDVYFreeAmidationNoneLinear4LCationicSyntheticNAMycobacterium smegmatisMycobacterium smegmatis RIF-susceptible MIC = > 1000mg/Lin vitro RAW 264.7 mouse macrophageNAHC50= > 2000 mg/L on Human RBCNA NAStimulate TNF-α production Disrupt the mycobacterial membraneNANANA201424411680
antitb_1608RR-6RRRRRRFreeAmidationNoneLinear5LCationicSyntheticNAMycobacterium smegmatisMycobacterium smegmatis RIF-susceptible MIC = 125 mg/Lin vitro RAW 264.7 mouse macrophageNAHC50= > 2000 mg/L on Human RBCNA NAStimulate TNF-α production Disrupt the mycobacterial membraneNANANA201424411680
antitb_1611TP-5RKDVYFreeAmidationNoneLinear4LCationicSyntheticNAMycobacterium smegmatisMycobacterium smegmatis RIF-ResistanceNAin vitroRAW 264.7 mouse macrophageNAHC50= > 2000 mg/L on Human RBCNA NAStimulate TNF-α production Disrupt the mycobacterial membraneNANANA201424411680
antitb_1612RR-6RRRRRRFreeAmidationNoneLinear5LCationicSyntheticNAMycobacterium smegmatisMycobacterium smegmatis RIF-ResistanceMIC = 125 mg/Lin vitroRAW 264.7 mouse macrophageNAHC50= > 2000 mg/L on Human RBCNA NAStimulate TNF-α production Disrupt the mycobacterial membraneNANANA201424411680