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Literature summary extracted from

  • de Jonge, B.L.; Walkup, G.K.; Lahiri, S.D.; Huynh, H.; Neckermann, G.; Utley, L.; Nash, T.J.; Brock, J.; San Martin, M.; Kutschke, A.; Johnstone, M.; Laganas, V.; Hajec, L.; Gu, R.F.; Ni, H.; Chen, B.; Hutchings, K.; Holt, E.; McKinney, D.; Gao, N.; Livchak, S.; Thresher, J.
    Discovery of inhibitors of 4-phosphopantetheine adenylyltransferase (PPAT) to validate PPAT as a target for antibacterial therapy (2013), Antimicrob. Agents Chemother., 57, 6005-6015.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.7.3 gene coaD, recombinant expression in Escherichia coli strain BL21(DE3) Homo sapiens
2.7.7.3 gene coaD, recombinant overexpression in Escherichia coli strain BL21(DE3) Escherichia coli
2.7.7.3 gene coaD, recombinant overexpression in Escherichia coli strain BL21(DE3) Haemophilus influenzae
2.7.7.3 gene coaD, recombinant overexpression in Escherichia coli strain BL21(DE3) Streptococcus mutans
2.7.7.3 gene coaD, recombinant overexpression of wild-type and mutant enzymes in Escherichia coli strain BL21(DE3) Staphylococcus aureus
2.7.7.3 gene coaD, recombinant overexpression of wild/type and mutant enzymes in Escherichia coli strain BL21 pLysS(DE3), overexpression of Streptococcus pneumoniae coaD in Streptococcus pneumoniae is achieved by driving expression from the galU promoter Streptococcus pneumoniae

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.7.3 enzyme from Staphylococcus aureus subsp. aureus MW2 in complex with inhibitors, vapour diffusion method, mixing of 0.0025 ml of protein solution with 0.0025 ml of reservoir solution containing 14% to 19% PEG 3350, 200 mM ammonium sulfate, and 0.1 M propionic acid cacodylate Bis-Tris propane buffer, pH 7.5, 20°C, 5-7 days, X-ray diffraction structure determination and analysis at 1.72-2.38 A resolution, molecular replacement and modelling of inhibitor binding Staphylococcus aureus

Protein Variants

EC Number Protein Variants Comment Organism
2.7.7.3 F8L the enzyme mutant is less sensitive to inhibition by compound D compared to the wild-type enzyme Streptococcus pneumoniae
2.7.7.3 N106H the enzyme mutant is less sensitive to inhibition by compound D compared to the wild-type enzyme Staphylococcus aureus
2.7.7.3 N106Y the enzyme mutant is less sensitive to inhibition by compound D compared to the wild-type enzyme Staphylococcus aureus
2.7.7.3 N107H the enzyme mutant is less sensitive to inhibition by compound D compared to the wild-type enzyme Streptococcus pneumoniae
2.7.7.3 T117N the enzyme mutant is less sensitive to inhibition by compound D compared to the wild-type enzyme Streptococcus pneumoniae
2.7.7.3 V136F the enzyme mutant is less sensitive to inhibition by compound D compared to the wild-type enzyme Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.7.3 (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Haemophilus influenzae
2.7.7.3 (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Homo sapiens
2.7.7.3 (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Staphylococcus aureus
2.7.7.3 (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Streptococcus pneumoniae
2.7.7.3 (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Haemophilus influenzae
2.7.7.3 (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Staphylococcus aureus
2.7.7.3 (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Streptococcus mutans
2.7.7.3 (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
-
 Streptococcus pneumoniae
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Enterococcus faecium
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Escherichia coli
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Haemophilus influenzae
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide slight inhibition in vivo Homo sapiens
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Staphylococcus aureus
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Streptococcus mutans
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Streptococcus pneumoniae
2.7.7.3 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
-
 Streptococcus pyogenes
2.7.7.3 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
-
 Escherichia coli
2.7.7.3 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
-
 Haemophilus influenzae
2.7.7.3 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
-
 Staphylococcus aureus
2.7.7.3 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
-
 Streptococcus pneumoniae
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid slight inhibition in vivo Enterococcus faecium
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
-
 Escherichia coli
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
-
 Haemophilus influenzae
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
-
 Homo sapiens
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
-
 Staphylococcus aureus
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
-
 Streptococcus pneumoniae
2.7.7.3 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
-
 Streptococcus pyogenes
2.7.7.3 additional information compound library screening, the series of reversible inhibitors show inhibition of cell growth of Gram-positive species but not of Candida albicans. MIC values, overview. Compounds HTS hit, A, B, C, and D show poor inhibition in vivo Candida albicans
2.7.7.3 additional information compound library screening, the potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species. MIC values, overview Enterococcus faecium
2.7.7.3 additional information compound library screening, the potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species. Levels of inhibitory activity of compounds against Escherichia coli PPAT are measured in the reverse direction, MIC values, overview Escherichia coli
2.7.7.3 additional information compound library screening, the potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species. Levels of inhibitory activity of compounds against Haemophilus influenzae PPAT are measured in the reverse direction, MIC values, overview Haemophilus influenzae
2.7.7.3 additional information compound library screening, the series of reversible inhibitors show inhibition of cell growth of Gram-positive species but no or only slight inhibition of the human A-549 tumor cells, MIC values, overview. levels of inhibitory activity of compounds against Homo sapiens PPAT are measured in the forward direction. Only compound C shows poor inhibition in vivo Homo sapiens
2.7.7.3 additional information compound library screening, mode-of-inhibition studies with Staphylococcus aureus PPAT demonstrate representatives of this series to be reversible inhibitors competitive versus phosphopantetheine and uncompetitive versus ATP, binding to the enzyme-ATP complex, overview. The potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species. Levels of inhibitory activity of compounds against Staphylococcus aureus PPAT are measured in the forward direction, MIC values, mechanism of inhibition, overview Staphylococcus aureus
2.7.7.3 additional information compound library screening, the potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species. Levels of inhibitory activity of compounds against Streptococcus mutans PPAT are measured in the reverse direction, MIC values, overview Streptococcus mutans
2.7.7.3 additional information ccompound library screening, mode-of-inhibition studies with Streptococcus pneumoniae PPAT demonstrate representatives of this series to be reversible inhibitors competitive versus phosphopantetheine and uncompetitive versus ATP, binding to the enzyme-ATP complex, overview. The potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species, killing kinetic assays using Staphylococcus aureus strains ARC516 and a LytA- for Streptococcus pneumoniae. Levels of inhibitory activity of compounds against Streptococcus pneumoniae PPAT are measured in the forward direction. MIC values, mechanism of inhibition, overview Streptococcus pneumoniae
2.7.7.3 additional information compound library screening, the potency of the series is optimized using structure-based design, resulting in inhibition of cell growth of Gram-positive species. MIC values, overview Streptococcus pyogenes

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.7.3 ATP + pantetheine 4'-phosphate Staphylococcus aureus
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Streptococcus pyogenes
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Enterococcus faecium
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Escherichia coli
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Homo sapiens
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Candida albicans
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Streptococcus pneumoniae
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Haemophilus influenzae
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Streptococcus mutans
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Enterococcus faecium ARC521
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Streptococcus pyogenes ARC838
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Haemophilus influenzae KW20
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Streptococcus mutans UA159
-
 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate Staphylococcus aureus RN4220
-
 diphosphate + 3'-dephospho-CoA
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.7.7.3 Candida albicans B9WCR8 strain CD36; gene coaD
-
2.7.7.3 Enterococcus faecium
-
 gene coaD
-
2.7.7.3 Enterococcus faecium ARC521
-
 gene coaD
-
2.7.7.3 Escherichia coli P0A6I6 MG1655, gene coaD
-
2.7.7.3 Haemophilus influenzae P44805 gene coaD
-
2.7.7.3 Haemophilus influenzae KW20 P44805 gene coaD
-
2.7.7.3 Homo sapiens Q06203 gene coaD
-
2.7.7.3 Staphylococcus aureus
-
 gene coaD
-
2.7.7.3 Staphylococcus aureus RN4220
-
 gene coaD
-
2.7.7.3 Streptococcus mutans Q8DVH2 gene coaD
-
2.7.7.3 Streptococcus mutans UA159 Q8DVH2 gene coaD
-
2.7.7.3 Streptococcus pneumoniae Q8DNE6 gene coaD
-
2.7.7.3 Streptococcus pyogenes
-
 gene coaD
-
2.7.7.3 Streptococcus pyogenes ARC838
-
 gene coaD
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.7.3 recombinant enzyme PPAT from Escherichia coli strain BL21(DE3) to over 95% purity Escherichia coli
2.7.7.3 recombinant enzyme PPAT from Escherichia coli strain BL21(DE3) to over 95% purity Homo sapiens
2.7.7.3 recombinant enzyme PPAT from Escherichia coli strain BL21(DE3) to over 95% purity Haemophilus influenzae
2.7.7.3 recombinant enzyme PPAT from Escherichia coli strain BL21(DE3) to over 95% purity Streptococcus mutans
2.7.7.3 recombinant wild-type and mutant PPAT enzymes from Escherichia coli strain BL21 pLysS(DE3) to over 95% purity Streptococcus pneumoniae
2.7.7.3 recombinant wild-type and mutant PPAT enzymes from Escherichia coli strain BL21(DE3) to over 90% purity Staphylococcus aureus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.7.3 A-549 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Staphylococcus aureus diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Streptococcus pyogenes diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Enterococcus faecium diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Escherichia coli diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Homo sapiens diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Candida albicans diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Streptococcus pneumoniae diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Haemophilus influenzae diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Streptococcus mutans diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Enterococcus faecium ARC521 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Streptococcus pyogenes ARC838 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Haemophilus influenzae KW20 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Streptococcus mutans UA159 diphosphate + 3'-dephospho-CoA
-
 r
2.7.7.3 ATP + pantetheine 4'-phosphate
-
 Staphylococcus aureus RN4220 diphosphate + 3'-dephospho-CoA
-
 r

Synonyms

EC Number Synonyms Comment Organism
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Staphylococcus aureus
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Streptococcus pyogenes
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Enterococcus faecium
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Escherichia coli
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Homo sapiens
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Candida albicans
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Streptococcus pneumoniae
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Haemophilus influenzae
2.7.7.3 4-phosphopantetheine adenylyltransferase
-
 Streptococcus mutans
2.7.7.3 PPAT
-
 Staphylococcus aureus
2.7.7.3 PPAT
-
 Streptococcus pyogenes
2.7.7.3 PPAT
-
 Enterococcus faecium
2.7.7.3 PPAT
-
 Escherichia coli
2.7.7.3 PPAT
-
 Homo sapiens
2.7.7.3 PPAT
-
 Candida albicans
2.7.7.3 PPAT
-
 Streptococcus pneumoniae
2.7.7.3 PPAT
-
 Haemophilus influenzae
2.7.7.3 PPAT
-
 Streptococcus mutans

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.7.3 22
-
 assay at room temperature Staphylococcus aureus
2.7.7.3 22
-
 assay at room temperature Streptococcus pyogenes
2.7.7.3 22
-
 assay at room temperature Enterococcus faecium
2.7.7.3 22
-
 assay at room temperature Escherichia coli
2.7.7.3 22
-
 assay at room temperature Homo sapiens
2.7.7.3 22
-
 assay at room temperature Candida albicans
2.7.7.3 22
-
 assay at room temperature Streptococcus pneumoniae
2.7.7.3 22
-
 assay at room temperature Haemophilus influenzae
2.7.7.3 22
-
 assay at room temperature Streptococcus mutans

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.7.3 7
-
 assay at Staphylococcus aureus
2.7.7.3 7
-
 assay at Streptococcus pyogenes
2.7.7.3 7
-
 assay at Enterococcus faecium
2.7.7.3 7
-
 assay at Escherichia coli
2.7.7.3 7
-
 assay at Homo sapiens
2.7.7.3 7
-
 assay at Candida albicans
2.7.7.3 7
-
 assay at Streptococcus pneumoniae
2.7.7.3 7
-
 assay at Haemophilus influenzae
2.7.7.3 7
-
 assay at Streptococcus mutans

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.7.3 0.000000065
-
 pH 7.0, 22°C, recombinant enzyme Streptococcus pneumoniae 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
2.7.7.3 0.00000013
-
 pH 7.0, 22°C, recombinant enzyme Streptococcus pneumoniae 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
2.7.7.3 0.00000041
-
 pH 7.0, 22°C, recombinant enzyme Staphylococcus aureus 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
2.7.7.3 0.00000087
-
 pH 7.0, 22°C, recombinant enzyme Staphylococcus aureus 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
2.7.7.3 0.0000026
-
 pH 7.0, 22°C, recombinant enzyme Streptococcus mutans 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
2.7.7.3 0.00004
-
 pH 7.0, 22°C, recombinant enzyme Streptococcus pneumoniae 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
2.7.7.3 0.000098
-
 pH 7.0, 22°C, recombinant enzyme Streptococcus mutans (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.00011
-
 pH 7.0, 22°C, recombinant enzyme Escherichia coli 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
2.7.7.3 0.00012
-
 pH 7.0, 22°C, recombinant enzyme Haemophilus influenzae 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
2.7.7.3 0.000205
-
 pH 7.0, 22°C, recombinant enzyme Streptococcus pneumoniae (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.00033
-
 pH 7.0, 22°C, recombinant enzyme Staphylococcus aureus (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.00033
-
 pH 7.0, 22°C, recombinant enzyme Escherichia coli 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
2.7.7.3 0.00049
-
 pH 7.0, 22°C, recombinant enzyme Staphylococcus aureus 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
2.7.7.3 0.00074
-
 pH 7.0, 22°C, recombinant enzyme Haemophilus influenzae 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
2.7.7.3 0.00086
-
 pH 7.0, 22°C, recombinant enzyme Haemophilus influenzae (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.0048
-
 pH 7.0, 22°C, recombinant enzyme Escherichia coli 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
2.7.7.3 0.005
-
 pH 7.0, 22°C, recombinant enzyme Homo sapiens (1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.0073
-
 pH 7.0, 22°C, recombinant enzyme Staphylococcus aureus (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.0088
-
 pH 7.0, 22°C, recombinant enzyme Haemophilus influenzae (1S,2S)-N-(3-chlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
2.7.7.3 0.0095
-
 pH 7.0, 22°C, recombinant enzyme Haemophilus influenzae 2-[(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)sulfanyl]-1H-imidazole-5-carboxylic acid
2.7.7.3 0.024
-
 pH 7.0, 22°C, recombinant enzyme Homo sapiens 2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
2.7.7.3 0.2
-
 pH 7.0, 22°C, recombinant enzyme Homo sapiens 3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid

General Information

EC Number General Information Comment Organism
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria Streptococcus pyogenes
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria Enterococcus faecium
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria Streptococcus mutans
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria, e.g. Escherichia coli strain ARC534, phenotype of enzyme knockout mutant Escherichia coli strain W3110, overview Escherichia coli
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria, e.g. of Haemophilus influenzae strain ATCC 51907 Haemophilus influenzae
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria, e.g. of Staphylococcus aureus strain ARC516 Staphylococcus aureus
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the bacteria, e.g. of Streptococcus pneumoniae strains D39 and ATCC 10813 Streptococcus pneumoniae
2.7.7.3 malfunction enzyme inhibition causes growth suppression of the cells Candida albicans