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Literature summary extracted from

  • Huang, W.; Zhang, Z.; Barros-Alvarez, X.; Koh, C.Y.; Ranade, R.M.; Gillespie, J.R.; Creason, S.A.; Shibata, S.; Verlinde, C.L.M.J.; Hol, W.G.J.; Buckner, F.S.; Fan, E.
    Structure-guided design of novel Trypanosoma brucei methionyl-tRNA synthetase inhibitors (2016), Eur. J. Med. Chem., 124, 1081-1092 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.10 (1R,3S)-3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) cyclohexanamine
-
Trypanosoma brucei
6.1.1.10 (R)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) piperidin-3-amine
-
Trypanosoma brucei
6.1.1.10 (R)-1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) pyrrolidin-3-amine
-
Trypanosoma brucei
6.1.1.10 (S)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) piperidin-3-amine
-
Trypanosoma brucei
6.1.1.10 (S)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorophenyl) piperidine-3-carboxamide
-
Trypanosoma brucei
6.1.1.10 (S)-1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) pyrrolidin-3-amine
-
Trypanosoma brucei
6.1.1.10 (S)-3,5-dichloro-N-(1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-yl)benzamide
-
Trypanosoma brucei
6.1.1.10 (S)-5-chloro-2-(3-((3,5-dichlorobenzyl)oxy)piperidin-1-yl)-1H-imidazo[4,5-b]pyridine
-
Trypanosoma brucei
6.1.1.10 1-(3-(1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
-
Trypanosoma brucei
6.1.1.10 1-(3-(4-chloro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
-
Trypanosoma brucei
6.1.1.10 1-(3-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
-
Trypanosoma brucei
6.1.1.10 1-(3-(5-chloro-1H-benzo[d]imidazol-2-yl) piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
-
Trypanosoma brucei
6.1.1.10 1-(3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
-
Trypanosoma brucei
6.1.1.10 1-(3-(5-chloro-6-fluoro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
-
Trypanosoma brucei
6.1.1.10 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)azepan-3-amine
-
Trypanosoma brucei
6.1.1.10 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)azetidin-3-amine
-
Trypanosoma brucei
6.1.1.10 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)piperidin-3-amine
-
Trypanosoma brucei
6.1.1.10 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)piperidin-4-amine
-
Trypanosoma brucei
6.1.1.10 2-((5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)thio)-N-(3,5-dichlorobenzyl) ethanamine
-
Trypanosoma brucei
6.1.1.10 2-(3,5-dichlorophenyl)-1-(3-(5-fluoro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethanone
-
Trypanosoma brucei
6.1.1.10 3,5-dichloro-N-((1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-yl)methyl)aniline
-
Trypanosoma brucei
6.1.1.10 3-(5-chloro-1H-benzo[d]imidazol-2-yl)-N-(3,5-dichlorobenzyl)cyclohexanamine
-
Trypanosoma brucei
6.1.1.10 3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) cyclohexanamine
-
Trypanosoma brucei
6.1.1.10 3-(5-chloro-3H-imidazo [4,5-b] pyridin-2-yl)-N-(3,5-dichlorobenzyl)propan-1-amine
-
Trypanosoma brucei
6.1.1.10 3-(6-chloro-1H-benzo[d]imidazol-2-yl)-N-(3,5-dichlorobenzyl) propan-1-amine
-
Trypanosoma brucei
6.1.1.10 5-chloro-2-(1-(3,5-dichlorophenethyl)piperidin-3-yl)-1H-imidazo[4,5-b]pyridine
-
Trypanosoma brucei
6.1.1.10 N1-(1H-benzimidazol-2-yl)-N3-[(3,5-dichlorophenyl)methyl]propane-1,3-diamine
-
Trypanosoma brucei
6.1.1.10 N1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N2-[(3,5-dichlorophenyl)methyl]-N1-methylethane-1,2-diamine
-
Trypanosoma brucei
6.1.1.10 N1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N2-(3,5-dichlorobenzyl) ethane-1,2-diamine
-
Trypanosoma brucei
6.1.1.10 N1-(6-chloro-1H-benzo[d]imidazol-2-yl)-N2-(3,5-dichlorobenzyl)ethane-1,2-diamine
-
Trypanosoma brucei
6.1.1.10 [3-(1H-benzimidazol-2-yl)piperidin-1-yl](2-methyl-1-benzofuran-5-yl)methanone 78% and 20% inhibition at 0.1 and 0.01 mM, respectively Trypanosoma brucei

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
6.1.1.10 ATP + L-methionine + tRNAMet Trypanosoma brucei
-
AMP + diphosphate + L-methionyl-tRNAMet
-
?
6.1.1.10 ATP + L-methionine + tRNAMet Trypanosoma brucei 927
-
AMP + diphosphate + L-methionyl-tRNAMet
-
?

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.10 Trypanosoma brucei Q38C91
-
-
6.1.1.10 Trypanosoma brucei 927 Q38C91
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.1.1.10 ATP + L-methionine + tRNAMet
-
Trypanosoma brucei AMP + diphosphate + L-methionyl-tRNAMet
-
?
6.1.1.10 ATP + L-methionine + tRNAMet
-
Trypanosoma brucei 927 AMP + diphosphate + L-methionyl-tRNAMet
-
?

Synonyms

EC Number Synonyms Comment Organism
6.1.1.10 methionyl-tRNA synthetase
-
Trypanosoma brucei
6.1.1.10 MetRS
-
Trypanosoma brucei

Cofactor

EC Number Cofactor Comment Organism Structure
6.1.1.10 ATP
-
Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei (S)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) piperidin-3-amine
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei (S)-1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) pyrrolidin-3-amine
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei N1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N2-[(3,5-dichlorophenyl)methyl]-N1-methylethane-1,2-diamine
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)piperidin-3-amine
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei 3,5-dichloro-N-((1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-yl)methyl)aniline
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei 3-(5-chloro-3H-imidazo [4,5-b] pyridin-2-yl)-N-(3,5-dichlorobenzyl)propan-1-amine
6.1.1.10 0.00005
-
pH and temperature not specified in the publication Trypanosoma brucei N1-(6-chloro-1H-benzo[d]imidazol-2-yl)-N2-(3,5-dichlorobenzyl)ethane-1,2-diamine
6.1.1.10 0.00006
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(3-(5-chloro-1H-benzo[d]imidazol-2-yl) piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
6.1.1.10 0.000085
-
pH and temperature not specified in the publication Trypanosoma brucei N1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N2-(3,5-dichlorobenzyl) ethane-1,2-diamine
6.1.1.10 0.000106
-
pH and temperature not specified in the publication Trypanosoma brucei (1R,3S)-3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) cyclohexanamine
6.1.1.10 0.000124
-
pH and temperature not specified in the publication Trypanosoma brucei 3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) cyclohexanamine
6.1.1.10 0.000138
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(3-(5-chloro-6-fluoro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
6.1.1.10 0.000184
-
pH and temperature not specified in the publication Trypanosoma brucei 2-(3,5-dichlorophenyl)-1-(3-(5-fluoro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethanone
6.1.1.10 0.000192
-
pH and temperature not specified in the publication Trypanosoma brucei (R)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) piperidin-3-amine
6.1.1.10 0.000196
-
pH and temperature not specified in the publication Trypanosoma brucei (S)-5-chloro-2-(3-((3,5-dichlorobenzyl)oxy)piperidin-1-yl)-1H-imidazo[4,5-b]pyridine
6.1.1.10 0.000243
-
pH and temperature not specified in the publication Trypanosoma brucei 3-(6-chloro-1H-benzo[d]imidazol-2-yl)-N-(3,5-dichlorobenzyl) propan-1-amine
6.1.1.10 0.000288
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(3-(1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
6.1.1.10 0.00058
-
pH and temperature not specified in the publication Trypanosoma brucei 3-(5-chloro-1H-benzo[d]imidazol-2-yl)-N-(3,5-dichlorobenzyl)cyclohexanamine
6.1.1.10 0.000682
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)azepan-3-amine
6.1.1.10 0.000696
-
pH and temperature not specified in the publication Trypanosoma brucei (R)-1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) pyrrolidin-3-amine
6.1.1.10 0.000812
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(3-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
6.1.1.10 0.000926
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(3-(4-chloro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
6.1.1.10 0.001054
-
pH and temperature not specified in the publication Trypanosoma brucei 2-((5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)thio)-N-(3,5-dichlorobenzyl) ethanamine
6.1.1.10 0.002166
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)azetidin-3-amine
6.1.1.10 0.00497
-
pH and temperature not specified in the publication Trypanosoma brucei 1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)piperidin-4-amine
6.1.1.10 0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Trypanosoma brucei (S)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorophenyl) piperidine-3-carboxamide
6.1.1.10 0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Trypanosoma brucei 5-chloro-2-(1-(3,5-dichlorophenethyl)piperidin-3-yl)-1H-imidazo[4,5-b]pyridine
6.1.1.10 0.01
-
pH and temperature not specified in the publication Trypanosoma brucei (S)-3,5-dichloro-N-(1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-yl)benzamide