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(2,3)-alpha-methylene benzylpenicillin
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modeling of enzyme-inhibitor complex
(2-phenylethyl)boronic acid
91% residual activity at 1 mM
(2R)-2-amino-7-oxo-7-[(4,4,4-trifluoro-3-oxobutan-2-yl)amino]heptanoic acid
i.e. D-alpha-aminopimelyl-(1,1,1-trifluoro-3-amino)butan-2-one
(3-aminophenyl)boronic acid
20% residual activity at 1 mM
(3-nitrophenyl)boronic acid
82% residual activity at 1 mM
(3H)benzylpenicillin
Streptomyces pneumoniae
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-
(3R,5R)-3-(furyl-2')-4-dethia-4-oxa-penam
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-
(3R,5R,6R)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam
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(3R,5R,6S)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam
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(3R,5S)-3-(furyl-2')-4-dethia-4-oxa-penam
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(3R,5S,6R)-3-benzyloxycarbonyl-6-methyl-4-dethia-4-oxa-penam
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(3R,5S,6R)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam
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(3S,5R)-3-(furyl-2')-4-dethia-4-oxa-penam
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-
(3S,5R,6S)-3-benzyloxycarbonyl-6-methyl-4-dethia-4-oxa-penam
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-
(3S,5R,6S)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam
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(3S,5S)-3-(furyl-2')-4-dethia-4-oxa-penam
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-
(3S,5S,6R)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam
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-
(4-phenoxyphenyl)boronic acid
98% residual activity at 1 mM
(5-acetylthiophen-2-yl)boronic acid
88% residual activity at 1 mM
(5-chlorothiophen-2-yl)boronic acid
91% residual activity at 1 mM
(5-cyanothiophen-2-yl)boronic acid
95% residual activity at 1 mM
(5-formylthiophen-2-yl)boronic acid
99% residual activity at 1 mM
(5R,6R)-6-[[(6S)-6-carboxy-6-(glycylamino)hexanoyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
-
-
(6R,7R)-3-[(acetyloxy)methyl]-7-[(6S)-6-carboxy-6-(glycylamino)hexanoyl]amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
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-
1-benzothiophen-2-ylboronic acid
86% residual activity at 1 mM
2,1-benzoxaborol-1(3H)-ol
45% residual activity at 1 mM
2,3-dimercapto-1-propane-sulfonic acid
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-
2,3-dimercapto-1-propanol
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-
3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid
38% residual activity at 0.5 mM
3-(acetylamino)-5-(dihydroxyboranyl)benzoic acid
50% residual activity at 1 mM
3-(benzoylamino)-5-(dihydroxyboranyl)benzoic acid
9% residual activity at 1 mM
3-(dihydroxyboranyl)-4-[(phenylacetyl)amino]benzoic acid
80% residual activity at 1 mM
3-(dihydroxyboranyl)-5-[(2,6-dimethoxybenzoyl)amino]benzoic acid
84% residual activity at 1 mM
3-(dihydroxyboranyl)-5-[(phenoxyacetyl)amino]benzoic acid
2% residual activity at 1 mM
3-(dihydroxyboranyl)-5-[(thiophen-2-ylacetyl)amino]benzoic acid
5% residual activity at 1 mM
3-(dihydroxyboranyl)-5-[(thiophen-2-ylcarbonyl)amino]benzoic acid
18% residual activity at 1 mM
3-(dihydroxyboryl)-5-(2-methoxybenzamido)benzoic acid
10% residual acvtivity at 1 mM
3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoic acid
3% residual acvtivity at 1 mM
3-(dihydroxyboryl)benzoic acid
20% residual acvtivity at 1 mM
3-(N-glycyl-L-cysteinyl)-N-ethylpropionamide
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-
3-(trifluoroacetyl)benzoic acid
60% residual activity at 1 mM
3-formylbenzoic acid
77% residual activity at 1 mM
4-(dihydroxyboranyl)benzoic acid
85% residual activity at 1 mM
4-chloromercuribenzoate
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complete inhibition at 1 mM
4-[(phenylacetyl)amino]-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid
81% residual activity at 1 mM
5-(dihydroxyboranyl)thiophene-2-carboxylic acid
57% residual activity at 1 mM
6-beta(alpha-N-acetyl-L-lysyl)-aminopenicillanic acid
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-
6-beta(D-alpha-aminopimelyl)-aminopenicillanic acid
6-beta(D-alpha-aminosuberyl)-aminopenicillanic acid
6-beta(N-acetyl-L-alanyl-gamma-D-glutamyl-L-alanyl)-aminopenicillanic acid
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7-(phenoxyacetamido)-3-desacetoxycephalosporamic acid
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7-beta(alpha-N-acetyl-L-lysyl)-aminocephalosporanic acid
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7-beta(D-alpha-aminopimelyl)-aminocephalosporanic acid
alpha-N-glycyl-epsilon-N-acetyl-L-lysine
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inhibits hydrolysis of 3-(N-glycyl-L-cysteinyl)-propanoyl-D-alanyl-D-thiolactate
arylakylidene imino-thiazolidin-4-ones 10
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86% inhibition
arylakylidene imino-thiazolidin-4-ones 11
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82% inhibition
arylakylidene imino-thiazolidin-4-ones 12
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64% inhibition
arylakylidene imino-thiazolidin-4-ones 13
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83% inhibition
arylakylidene imino-thiazolidin-4-ones 16
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100% inhibition
arylakylidene imino-thiazolidin-4-ones 17
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100% inhibition
arylakylidene imino-thiazolidin-4-ones 18
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96% inhibition
arylakylidene imino-thiazolidin-4-ones 19
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84% inhibition
arylakylidene imino-thiazolidin-4-ones 5
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89% inhibition
arylakylidene imino-thiazolidin-4-ones 6
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92% inhibition
arylakylidene imino-thiazolidin-4-ones 8
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99% inhibition
arylakylidene imino-thiazolidin-4-ones 9
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85% inhibition
arylalkylidene rhodanine derivative 1
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88% inhibition
arylalkylidene rhodanine derivative 2
arylalkylidene rhodanine derivative 3
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83% inhibition
arylalkylidene rhodanine derivative 4
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95% inhibition
ayercillin
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dipeptide-releasing activity is penicillin sensitive
biphenyl-4,4'-diyldiboronic acid
97% residual activity at 0.1 mM
Boc-gamma-D-Glu-L-Lys-(Cbz)-D-boroAla-(-)-pinanediol
effective inhibitor of the D-alanine CPase activity of PBP5
cephalosporin C
classical non-specific beta-lactam
cetyltrimethylammonium bromide
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D-Ala(P,O)D-Ala
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acts as slow binding inhibitor
D-Ala(P,O)D-Phe
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acts as slow binding inhibitor
D-alpha-phenylpropionate
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Delta2-(and Delta3)-Deacetoxy-7-phenylacetamidocephalosporanates
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diisopropyl fluorophosphate
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1 mM, 28% inhibition
EDTA
4 mM, complete loss of activity. Ativity may be restored in presence of 8 mM Zn2+
epsilon-N-glycyl-alpha-N-acetyl-L-alanyl-D-isoglutaminyl-L-lysine
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inhibits hydrolysis of 3-(N-glycyl-L-cysteinyl)-propanoyl-D-alanyl-D-thiolactate
formaldehyde
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1 mM, 53% inhibition
iodoacetamide
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1 mM, 20% inhibition
Mercaptosuccinic acid
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N,N-diacetyl-L-Lys-D-Ala-D-Ala
Streptomyces pneumoniae
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inhibition of PBP3 by its own substrate above a ligand concentration of 15 mM
N-(glycyl)-D,L-alpha-aminocaprylic acid
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inhibits hydrolysis of 3-(N-glycyl-L-cysteinyl)-propanoyl-D-alanyl-D-thiolactate
N-benzoyl-beta-sultam
time-dependent, irreversible active site directed inhibitor, the rate of inactivation is first order with respect to beta-sultam concentration and second order rate constants show dependence on pH
N-Chlorosuccinimide
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1 mM, 50% inhibition
N-p-methoxy-beta-sultam
least effective inhibitor
Nalpha-tert-butoxycarbonyl-Nepsilon-benzyloxycarbonyl-L-Lys-D-Ala-D-Ala
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substrate inhibition above 30 mM
NEM
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1 mM, complete inhibition
Oxyimino-DELTA3-cephalosporins
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p-hydroxymercuribenzoate
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1 mM, complete inhibition
phenoxymethylpenicillin
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phenyl glycyl-L-alpha-aminopimelyl-epsilon-(D-2-aminoethyl)phosphonate
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thiophen-2-ylboronic acid
88% residual activity at 1 mM
Vancomycin
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vancomycin derivatives inhibit the glycosyl transferase activity
[3-([[5-(dimethylamino)naphthalen-1-yl]sulfonyl]amino)phenyl]boronic acid
60% residual activity at 0.5 mM
[3-[(2,6-dimethoxybenzoyl)amino]-5-(methoxycarbonyl)thiophen-2-yl]boronic acid
98% residual activity at 1 mM
6-beta(D-alpha-aminopimelyl)-aminopenicillanic acid
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6-beta(D-alpha-aminopimelyl)-aminopenicillanic acid
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6-beta(D-alpha-aminosuberyl)-aminopenicillanic acid
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6-beta(D-alpha-aminosuberyl)-aminopenicillanic acid
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-
7-beta(D-alpha-aminopimelyl)-aminocephalosporanic acid
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7-beta(D-alpha-aminopimelyl)-aminocephalosporanic acid
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ampicillin
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complete inhibition at 0.57 mM, 95% inhibition at 0.285 mM
arylalkylidene rhodanine derivative 2
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95% inhibition
arylalkylidene rhodanine derivative 2
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94% inhibition
arylalkylidene rhodanine derivative 2
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75% inhibition
benzylpenicillin
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ester-linked to serins
benzylpenicillin
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IC50: 0.00002 mg/ml, inhibition of the enzyme influences production of peptidoglycan precursors internally
benzylpenicillin
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80% inhibition at 0.1 mg/ml
benzylpenicillin
classical non-specific beta-lactam
beta-lactam
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R39 has a high beta-lactam binding activity
beta-lactams
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kinetic constants
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beta-lactams
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kinetic constants
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Ca2+
1 mM, no residual activity
cephalosporin
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cephalosporin
with glycyl-L-alpha-amino-epsilon-pimelyl side-chain, this beta lactam might be a better antibiotic than a non-specific counterpart
cephalothin
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-
Methicillin
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-
Mg2+
1 mM, no residual activity
Moenomycin
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inhibits the glycosyl transferase activity
nocardicin A
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-
Oxyimino-DELTA3-cephalosporins
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syn- and anti-isomers
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Oxyimino-DELTA3-cephalosporins
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syn- and anti-isomers
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penicillin
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kinetic model of interaction
penicillin
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binds covalently to Ser36, Bacillus subtilis, Bacillus stearothermophilus
penicillin
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binds covalently to Ser36, Bacillus subtilis, Bacillus stearothermophilus
penicillin
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the enzyme is sensitive to inhibition, penicillin-binding profile during development of spores, overview
penicillin
Streptomyces pneumoniae
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-
penicillin
-
kinetic model of interaction
penicillin
having the glycyl-L-alpha-amino-epsilon-pimelyl side-chain of Streptomyces strain R61 peptidoglycan, this beta lactam might be the perfect antibiotic as compared to a non-specific counterpart
penicillin G
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100% inhibition
penicillin G
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100% inhibition
penicillin G
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100% inhibition
phenylboronic acid
50% residual activity at 0.5 mM
phenylboronic acid
-
1 mM, 26% inhibition
piperacillin
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-
sulfazecine
-
-
Zn2+
-
-
Zn2+
1 mM, no residual activity
additional information
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no significant inhibition by arylalkylidene rhodanine derivative 1 and 3 respectively and arylakylidene imino-thiazolidin-4-ones 6, 8, 13, 16, 17 and 19 respectively
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additional information
not inhibited by methyl 3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoate
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additional information
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no inhibition: penicillin G, ampicillin, cephalosporin C
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additional information
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inhibition studies
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additional information
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no significant inhibition by arylakylidene imino-thiazolidin-4-ones 7, 14 and 15 respectively
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additional information
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no inhibition: EDTA
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additional information
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serine enzyme not inhibited by PMSF
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additional information
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no inhibition: EDTA
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additional information
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no inhibition: EDTA
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additional information
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inhibition studies
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additional information
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no significant inhibition by arylalkylidene rhodanine derivative 1, 3 and 4 respectively and arylakylidene imino-thiazolidin-4-ones 5 to 19
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