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Literature summary extracted from

  • Pohlmann, J.
    Phenylalanyl-tRNA synthetase as a target for potential new antibacterial agents (2004), Drugs Future, 29, 243-251.
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.20 (2R,3R,3aS,5aR,10R,10aR)-N-(3,4-dichlorophenyl)-10-hydroxy-4-oxo-2-phenyl-2,3,3a,4,5a,10-hexahydrofuro[2,3-c]indeno[1,2-b]furan-3-carboxamide
-
 Escherichia coli
6.1.1.20 (2R,3R,3aS,5aR,10S,10aR)-N-(3,4-dichlorophenyl)-10-hydroxy-4-oxo-2-phenyl-2,3,3a,4,5a,10-hexahydrofuro[2,3-c]indeno[1,2-b]furan-3-carboxamide
-
 Escherichia coli
6.1.1.20 (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.002 mM Enterococcus faecalis
6.1.1.20 (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.00017 mM Escherichia coli
6.1.1.20 (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.0016 mM Staphylococcus aureus
6.1.1.20 (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one IC50: 600 nM Enterococcus faecalis
6.1.1.20 (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one IC50: 10 nM Escherichia coli
6.1.1.20 (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one IC50: 70 nM Staphylococcus aureus
6.1.1.20 (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 5 nM Enterococcus faecalis
6.1.1.20 (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 130 nM Escherichia coli
6.1.1.20 (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 4 nM Staphylococcus aureus
6.1.1.20 (3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 820 nM Enterococcus faecalis
6.1.1.20 (3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 3200 nM Escherichia coli
6.1.1.20 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea IC50: 15 nM Escherichia coli
6.1.1.20 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea IC50: 15 nM Haemophilus influenzae
6.1.1.20 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea IC50: 50 nM Streptococcus pneumoniae
6.1.1.20 2-phenylacetamidine competitive with respect to phenylalanine Escherichia coli
6.1.1.20 benzylguanidine competitive with respect to phenylalanine Escherichia coli
6.1.1.20 L-phenylalanyl-adenylate
-
 Escherichia coli
6.1.1.20 N-benzyl-D-amphetamine most potent competitive inhibitor, selectivity for bacterial enzyme Escherichia coli
6.1.1.20 N-benzylbenzamidine competitive with respect to phenylalanine Escherichia coli
6.1.1.20 N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide IC50: 8 nM Escherichia coli
6.1.1.20 N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide IC50: 8 nM Haemophilus influenzae
6.1.1.20 N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide IC50: 50 nM Staphylococcus aureus
6.1.1.20 ochratoxin A
-
 Escherichia coli

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
6.1.1.20 0.05
-
 L-Phe
-
 Staphylococcus aureus
6.1.1.20 0.05
-
 L-Phe
-
 Haemophilus influenzae
6.1.1.20 0.05
-
 L-Phe
-
 Escherichia coli
6.1.1.20 0.05
-
 L-Phe
-
 Enterococcus faecalis
6.1.1.20 0.05
-
 L-Phe
-
 Streptococcus pneumoniae

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.20 Enterococcus faecalis
-
-
-
6.1.1.20 Escherichia coli
-
-
-
6.1.1.20 Haemophilus influenzae
-
-
-
6.1.1.20 Staphylococcus aureus
-
-
-
6.1.1.20 Streptococcus pneumoniae
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.1.1.20 ATP + L-Phe + tRNAPhe
-
 Enterococcus faecalis AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?
6.1.1.20 ATP + L-phenylalanine + tRNAPhe
-
 Staphylococcus aureus AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?
6.1.1.20 ATP + L-phenylalanine + tRNAPhe
-
 Haemophilus influenzae AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?
6.1.1.20 ATP + L-phenylalanine + tRNAPhe
-
 Streptococcus pneumoniae AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.1.1.20 Phe-RS
-
 Staphylococcus aureus
6.1.1.20 Phe-RS
-
 Haemophilus influenzae
6.1.1.20 Phe-RS
-
 Escherichia coli
6.1.1.20 Phe-RS
-
 Enterococcus faecalis
6.1.1.20 Phe-RS
-
 Streptococcus pneumoniae

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
6.1.1.20 0.00014
-
 N-benzyl-D-amphetamine
-
 Escherichia coli
6.1.1.20 0.058
-
 N-benzylbenzamidine
-
 Escherichia coli
6.1.1.20 0.077
-
 benzylguanidine
-
 Escherichia coli
6.1.1.20 0.23
-
 2-phenylacetamidine
-
 Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.1.1.20 0.000004
-
 IC50: 4 nM Staphylococcus aureus (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
6.1.1.20 0.000005
-
 IC50: 5 nM Enterococcus faecalis (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
6.1.1.20 0.000008
-
 IC50: 8 nM Haemophilus influenzae N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide
6.1.1.20 0.000008
-
 IC50: 8 nM Escherichia coli N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide
6.1.1.20 0.00001
-
 IC50: 10 nM Escherichia coli (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
6.1.1.20 0.000015
-
 IC50: 15 nM Haemophilus influenzae 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea
6.1.1.20 0.000015
-
 IC50: 15 nM Escherichia coli 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea
6.1.1.20 0.00005
-
 IC50: 50 nM Staphylococcus aureus N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide
6.1.1.20 0.00005
-
 IC50: 50 nM Streptococcus pneumoniae 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea
6.1.1.20 0.00007
-
 IC50: 70 nM Staphylococcus aureus (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
6.1.1.20 0.00013
-
 IC50: 130 nM Escherichia coli (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
6.1.1.20 0.00017
-
 competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.00017 mM Escherichia coli (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
6.1.1.20 0.0006
-
 IC50: 600 nM Enterococcus faecalis (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
6.1.1.20 0.00082
-
 IC50: 820 nM Enterococcus faecalis (3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
6.1.1.20 0.0016
-
 competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.0016 mM Staphylococcus aureus (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
6.1.1.20 0.002
-
 competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.002 mM Enterococcus faecalis (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
6.1.1.20 0.0032
-
 IC50: 3200 nM Escherichia coli (3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone